☆ 4.5 Article

New pyrimidine/thiazole hybrids endowed with analgesic, anti-inflammatory, and lower cardiotoxic activities: Design, synthesis, and COX-2/sEH dual inhibition

ARCHIV DER PHARMAZIE (2022)

期刊

ARCHIV DER PHARMAZIE

卷 355, 期 7, 页码 -

出版社

WILEY-V C H VERLAG GMBH

DOI: 10.1002/ardp.202200024

关键词

anti-inflammatory; COX-2; pyrimidine; sEH; thiazole; ulcer

类别

Chemistry, Medicinal Chemistry, Multidisciplinary Pharmacology & Pharmacy

向作者/读者索取更多资源

Protocol

Reagent

智能总结 New
摘要

A new series of pyrimidine/thiazole hybrids 7a-p were synthesized as selective COX-2/sEH inhibitors with analgesic and anti-inflammatory effects, and lower cardiotoxicity effects. Some hybrids showed the greatest COX-2-inhibitory activity and were discovered to be the most potent dual COX-2/sEH inhibitors, with improved ulcerogenic and cardioprotective properties.

Some cyclooxygenase (COX)-2 selective medications were withdrawn from the market just a few years after their production due to cardiovascular side effects. In this study, a new series of pyrimidine/thiazole hybrids 7a-p was synthesized as selective COX-2/soluble epoxide hydrolase (sEH) inhibitors with analgesic and anti-inflammatory effects, and lower cardiotoxicity effects. The target compounds were synthesized and in vitro tested against COX-1, COX-2, and sEH enzymes. Hybrids 7j, 7k, and 7i showed the greatest COX-2-inhibitory activity and were discovered to be the most potent dual COX-2/sEH inhibitors. In vivo tests revealed that these hybrids were the most active analgesic/anti-inflammatory agents, with improved ulcerogenic and cardioprotective properties. Finally, the most active dual inhibitors were docked into COX-2/sEH active regions to explain their binding mechanisms.

作者

我是这篇论文的作者

点击您的名字以认领此论文并将其添加到您的个人资料中。

评论

主要评分

4.5

评分不足

次要评分

新颖性

-

重要性

-

科学严谨性

-

评价这篇论文

推荐

Article Biochemistry & Molecular Biology

Design, synthesis, and biological evaluation of new pyrimidine-5-carbonitrile derivatives bearing 1,3-thiazole moiety as novel anti-inflammatory EGFR inhibitors with cardiac safety profile

Salah A. Abdel-Aziz, Ehab S. Taher, Ping Lan, Gihan F. Asaad, Hesham A. M. Gomaa, Nawal A. El-Koussi, Bahaa G. M. Youssif

Summary: A new series of pyrimidine-5-carbonitrile derivatives carrying the 1,3-thiazole moiety have been designed and synthesized as novel anti-inflammatory EGFR inhibitors with cardiac and gastric safety profiles. These compounds showed potent and selective COX-2 inhibition, significant in-vivo anti-inflammatory effects, and superior gastric safety profiles compared to meloxicam. Additionally, they exhibited cardiovascular safety, anti-proliferative effects, and superior inhibitory activity against wild-type EGFR.

BIOORGANIC CHEMISTRY (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

Novel 1,5-diaryl pyrazole-3-carboxamides as selective COX-2/sEH inhibitors with analgesic, anti-inflammatory, and lower cardiotoxicity effects

O. M. Hendawy, Hesham A. M. Gomaa, Sami Alzarea, Mutariah S. Alshammari, Fatma A. M. Mohamed, Yaser A. Mostafa, Ahmed H. Abdelazeem, Mostafa H. Abdelrahman, Laurent Trembleau, Bahaa G. M. Youssif

Summary: New series of COX-2/sEH inhibitors were synthesized to replace withdrawn COX-2 selective drugs, with promising analgesic, anti-inflammatory effects and lower cardiotoxicity. Compounds 20, 22, and 29 showed significant COX-2 inhibitory activity and were the most potent dual COX-2/sEH inhibitors, demonstrating good analgesic/anti-inflammatory effects and cardioprotective properties in vivo studies.

BIOORGANIC CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects

Yufei Han, Desheng Huang, Sicong Xu, Lingling Li, Ye Tian, Shuo Li, Cong Chen, Yingxiu Li, Yanping Sun, Yunlei Hou, Yongjun Sun, Mingze Qin, Ping Gong, Zibin Gao, Yanfang Zhao

Summary: Inhibition of soluble epoxide hydrolase (sEH) represents a promising therapeutic strategy for inflammation treatment. Through the design of novel benzo[d]thiazol derivatives, compounds 15a and 18d were identified as potential sEH inhibitors with significant anti-inflammatory effects in animal models, thus warranting further development as potential drug candidates.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design and synthesis of pyrimidine-5-carbonitrile hybrids as COX-2 inhibitors: Anti-inflammatory activity, ulcerogenic liability, histopathological and docking studies

Abdallah M. Alfayomy, Salah A. Abdel-Aziz, Adel A. Marzouk, Montaser Sh. A. Shaykoon, Atsushi Narumi, Hiroyuki Konno, Sahar M. Abou-Seri, Fatma A. F. Ragab

Summary: Two new series of 1,3,4-oxadiazole and coumarin derivatives based on pyrimidine-5-carbonitrile scaffold were synthesized and evaluated for their COX-1/COX-2 inhibitory activity. Some compounds showed potent COX-2 inhibition and in vivo anti-inflammatory activity, with certain derivatives displaying superior efficacy and safety profile compared to the reference drug celecoxib. Molecular docking studies indicated similar binding interactions of select compounds 10c, 10j, and 14e as selective COX-2 inhibitors, with a higher potential for accessing the selectivity side pocket.

BIOORGANIC CHEMISTRY (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

New pyrazolyl-thiazolidinone/thiazole derivatives as celecoxib/dasatinib analogues with selective COX-2, HER-2 and EGFR inhibitory effects: design, synthesis, anti-inflammatory/anti-proliferative activities, apoptosis, molecular modelling and ADME studies

Wael A. A. Fadaly, Taha H. Zidan, Nesma M. Kahk, Fatma E. A. Mohamed, Marwa M. Abdelhakeem, Rehab G. Khalil, Mohamed T. M. Nemr

Summary: Two new series of pyrazolyl-thiazolidinone/thiazole derivatives were synthesized, which showed inhibitory activities against COX-2, MCF-7, A549, EGFR, and HER-2.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2023)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design, synthesis and mechanistic study of novel diarylpyrazole derivatives as anti-inflammatory agents with reduced cardiovascular side effects

Noha H. Amin, Mohammed I. A. Hamed, Maha M. Abdel-Fattah, Ahmed H. A. Abusabaa, Mohammed T. El-Saadi

Summary: Novel diarylpyrazole derivatives were synthesized, evaluated for dual COX-2/sEH inhibitory activities, and showed promising results as anti-inflammatory and analgesic agents with improved cardiovascular safety profiles. Compounds 6d and 11f exhibited excellent inhibitory activities against both COX-2 and sEH.

BIOORGANIC CHEMISTRY (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

Discovery of 5-Methylthiazole-Thiazolidinone Conjugates as Potential Anti-Inflammatory Agents: Molecular Target Identification and In Silico Studies

Michelyne Haroun, Anthi Petrou, Christophe Tratrat, Aggeliki Kolokotroni, Maria Fesatidou, Panagiotis Zagaliotis, Antonis Gavalas, Katharigatta N. Venugopala, Nagaraja Sreeharsha, Anroop B. Nair, Heba Sadek Elsewedy, Athina Geronikaki

Summary: This study evaluated the anti-inflammatory activity of a series of previously synthesized compounds and found that some of them showed better activity than the reference drug. Structure-activity relationship analysis revealed that both the nature and position of the substituent in the benzene ring influenced the activity of the compounds. Further investigation identified COX-1 inhibition as the main mechanism of action for the anti-inflammatory activity of these compounds.

MOLECULES (2022)

添加到收藏夹

Article Chemistry, Physical

Design, synthesis and anti-inflammatory/analgesic evaluation of novel di-substituted urea derivatives bearing diaryl-1,2,4-triazole with dual COX-2/sEH inhibitory activities

Ahmed H. Abdelazeem, Asmaa G. Safi El-Din, Hany H. Arab, Mohammed T. El-Saadi, Samir M. El-Moghazy, Noha H. Amin

Summary: Two novel series of compounds were synthesized and evaluated in vitro and in vivo, with compounds 10e and 10c showing the highest activity against COX-2/sEH enzymes. In vivo screening assays confirmed their superior anti-inflammatory and analgesic activity compared to other derivatives.

JOURNAL OF MOLECULAR STRUCTURE (2021)

添加到收藏夹

Article Chemistry, Physical

Synthesis, characterization, DFT, docking studies and molecular dynamics of some 3-phenyl-5-furan isoxazole derivatives as anti-inflammatory and anti-ulcer agents

H. M. Pallavi, Fares Hezam Al-Ostoot, Hamse Kameshwar Vivek, Shaukath Ara Khanum

Summary: This study synthesized isoxazole derivatives with therapeutic and anti-inflammatory potential and conducted detailed physical-chemical and biological evaluations. Compound (5f) showed comparable biological activity to the standard drug omeprazole in in-vitro studies. In addition, the bioavailability and toxicity of compound (5f) were evaluated through methods such as molecular docking and molecular dynamics.

JOURNAL OF MOLECULAR STRUCTURE (2022)

添加到收藏夹

Review Pharmacology & Pharmacy

Recent development on COX-2 inhibitors as promising anti-inflammatory agents: The past 10 years

Zhiran Ju, Menglan Li, Junde Xu, Daniel C. Howell, Zhiyun Li, Fen-Er Chen

Summary: Cyclooxygenases play a vital role in inflammation, but currently used anti-inflammatory drugs have associated adverse effects. Researchers are searching for novel selective COX-2 inhibitors.

ACTA PHARMACEUTICA SINICA B (2022)

添加到收藏夹

Article Chemistry, Physical

New quinoline/1,2,4-triazole hybrids as dual inhibitors of COX-2/5-LOX and inflammatory cytokines: Design, synthesis, and docking study

Aliaa M. Mohassab, Heba A. Hassan, Dalia Abdelhamid, Ahmed M. Gouda, Hesham A. M. Gomaa, Bahaa G. M. Youssif, Mohamed O. Radwan, Mikako Fujita, Masami Otsuka, Mohamed Abdel-Aziz

Summary: A novel series of quinoline/1,2,4-triazole hybrids were synthesized and evaluated as dual COX-2/5-LOX inhibitors. Compounds 6e, 6i, and 7e showed high potency and selectivity for inhibiting COX-2, consistent with the in vivo anti-inflammatory activity. Molecular docking analysis revealed high binding affinities towards COX-2, supporting their potential as anti-inflammatory agents.

JOURNAL OF MOLECULAR STRUCTURE (2021)

添加到收藏夹

Article Chemistry, Multidisciplinary

Supramolecular nanofiber of indomethacin derivative confers highly cyclooxygenase-2 (COX-2) selectivity and boosts anti-inflammatory efficacy

Deqing Lin, Xiaoning Xu, Lin Chen, Lei Chen, Mengyun Deng, Jinrun Chen, Zhibin Ren, Lei Lei, Jiaqing Wang, Jie Deng, Xingyi Li

Summary: A facile method for converting carboxylate-containing indomethacin into a cyclooxygenase-2 selective inhibitor via the amidation of an unnatural peptide sequence is reported. The resulting indomethacin amides have high selectivity for COX-2 and can self-assemble into a supramolecular hydrogel for boosting anti-inflammatory efficacy.

JOURNAL OF CONTROLLED RELEASE (2023)

添加到收藏夹

Article Chemistry, Physical

New 2-aminobenzothiazole derivatives: Design, synthesis, anti-inflammatory and ulcerogenicity evaluation

Sara S. Awaad, Mona O. Sarhan, Walaa R. Mahmoud, Tamer Nasr, Riham F. George, Hanan H. Georgey

Summary: Two series of twenty benzothiazole amide derivatives were synthesized and screened for their anti-inflammatory activity and gastric ulcerogenicity. Compounds 3h and 6a showed the most potent anti-inflammatory activity with high gastrointestinal tolerability. In vitro selectivity testing demonstrated that compound 6a had the best selectivity index among the investigated compounds.

JOURNAL OF MOLECULAR STRUCTURE (2023)

添加到收藏夹

Article Chemistry, Medicinal

New indomethacin analogs as selective COX-2 inhibitors: Synthesis, COX-1/2 inhibitory activity, anti-inflammatory, ulcerogenicity, histopathological, and docking studies

Khaled R. A. Abdellatif, Eman K. A. Abdelall, Heba A. H. Elshemy, El-Shaymaa El-Nahass, Maha M. Abdel-Fattah, Yasmin Y. M. Abdelgawad

Summary: New indomethacin analogs were synthesized to improve selectivity and reduce ulcer liability. The compounds showed higher potency and selectivity against COX-2 compared to celecoxib, with some analogs demonstrating good anti-inflammatory activity and safety profiles. Compound 5 emerged as a promising anti-inflammatory lead compound with potential for further development.

ARCHIV DER PHARMAZIE (2021)

添加到收藏夹

Article Chemistry, Multidisciplinary

Design, synthesis, characterization and analysis of anti-inflammatory properties of novel N-(benzo[d]thiazol-2-yl)-2-[phenyl(2-(piperidin-1-yl) ethylamino] benzamides and N-(benzo[d]thiazol-2-yl)-2-[phenyl (2-morpholino) ethylamino] benzamides derivatives through in vitro and in silico approach

Mahima Jyothi, V. Lakshmi Ranganatha, Hussien Ahmed Khamees, M. J. Nagesh Khadri, Shaukath Ara Khanum

Summary: A series of novel N-(benzo[d]thiazol-2-yl)-2-[phenyl(2-(piperidin-1-yl) ethylamino] benzamides and N-(benzo[d]thiazol-2-yl)-2-[phenyl(2-morpholino) ethylamino] benzamides derivatives were successfully synthesized and evaluated for their anti-inflammatory activity. Compounds with a methoxy group at the sixth position in the benzothiazole ring appended with piperidine and morpholine moieties showed the highest COX-1 inhibition and excellent COX-2 selectivity.

JOURNAL OF THE IRANIAN CHEMICAL SOCIETY (2023)

添加到收藏夹

Article Chemistry, Medicinal

New 1,3,4-oxadiazole-chalcone/benzimidazole hybrids as potent antiproliferative agents

Fatma Fouad Hagar, Samar H. Abbas, Dalia Abdelhamid, Hesham A. M. Gomaa, Bahaa G. M. Youssif, Mohamed Abdel-Aziz

Summary: A series of new 1,3,4-oxadiazole-chalcone/benzimidazole hybrids were synthesized and investigated for their antiproliferative activities. Compounds 9g-i and their oxygen isosteres, 10f-h, exhibited promising antiproliferative activities with IC50 values ranging from 0.80 to 2.27 μM.

ARCHIV DER PHARMAZIE (2023)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of new cyanopyridine/chalcone hybrids as dual inhibitors of EGFR/BRAFV600E with promising antiproliferative properties

Hesham A. Abou-Zied, Eman A. M. Beshr, Hesham A. M. Gomaa, Yaser A. Mostafa, Bahaa G. M. Youssif, Alaa M. Hayallah, Mohamed Abdel-Aziz

Summary: Dual EGFR and BRAF(V600E) inhibitors have been developed, showing strong antiproliferative activity and dual inhibition activity on EGFR and BRAF(V600E) in vitro.

ARCHIV DER PHARMAZIE (2023)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design, synthesis, and modelling study of new 1,2,3-triazole/chalcone hybrids with antiproliferative action as epidermal growth factor receptor inhibitors

Mohamed T. -E. Maghraby, Ola I. A. Salem, Bahaa G. M. Youssif, Mahmoud M. Sheha

Summary: A novel series of 1,2,3-triazole/chalcone hybrids were synthesized and evaluated for their cytotoxic activity and EGFR/BRAF inhibitory effects. Compound 6d showed the highest antiproliferative activity and was found to be a potent EGFR inhibitor. Additionally, it exhibited modest BRAF inhibitory action and caused cell cycle arrest at the G1 transition phase.

CHEMICAL BIOLOGY & DRUG DESIGN (2023)

添加到收藏夹

Article Biochemistry & Molecular Biology

Novel piperine-carboximidamide hybrids: design, synthesis, and antiproliferative activity via a multi-targeted inhibitory pathway

Lamya H. Al-Wahaibi, Mohamed A. Mahmoud, Yaser A. Mostafa, Ali E. Raslan, Bahaa G. M. Youssif

Summary: A new series of piperine-carboximidamide hybrids were developed as cytotoxic agents targeting EGFR, BRAF, and CDK2, and showed promising antiproliferative activity. Several compounds exhibited potent inhibitory effects on cancer cell proliferation, specifically targeting EGFR, BRAFV600E, and CDK2. The study also highlighted the importance of molecular docking and in silico ADME/pharmacokinetic analysis in drug design.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2023)

添加到收藏夹

Article Chemistry, Physical

Novel fluoroquinolone hybrids as dual DNA gyrase and urease inhibitors with potential antibacterial activity: Design, synthesis, and biological evaluation

Salah A. Abdel-Aziz, Katarina Cirnski, Jennifer Herrmann, Mohamed A. . A. . Abdel-Aal, Bahaa G. M. Youssif, Ola I. A. Salem

Summary: Fluoroquinolone compounds combined with thiouracil and thioxopyrimidine derivatives exhibit antibacterial, DNA gyrase, and urease inhibitory activities, with high purity and potency.

JOURNAL OF MOLECULAR STRUCTURE (2023)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design, Synthesis, and Antiproliferative Activity of New 5-Chloro-indole-2-carboxylate and Pyrrolo[3,4-b]indol-3-one Derivatives as Potent Inhibitors of EGFRT790M/BRAFV600E Pathways

Lamya H. Al-Wahaibi, Anber F. Mohammed, Mostafa H. Abdelrahman, Laurent Trembleau, Bahaa G. M. Youssif

Summary: This study presents the development of a novel series of derivatives that act as potent inhibitors of mutant EGFR/BRAF pathways with antiproliferative activity, suggesting their potential as targets for anticancer drug development.

MOLECULES (2023)

添加到收藏夹

Article Chemistry, Physical

Design, synthesis and antimicrobial activity of novel quinoline-2-one hybrids as promising DNA gyrase and topoisomerase IV inhibitors

Mohammed A. I. Elbastawesy, Fatma A. M. Mohamed, Islam Zaki, Mohammed Issa Alahmdi, Seham S. Alzahrani, Hayat Ali Alzahrani, Hesham A. M. Gomaa, Bahaa G. M. Youssif

Summary: A new series of quinoline-2-one Schiff-base hybrids were synthesized and characterized. The compounds were screened for antimicrobial activity and compound 6c showed significant inhibitory effects against B. subtilis, E. coli, and S. aureus. It also exhibited inhibitory activity against E. coli topoisomerase IV and DNA gyrase.

JOURNAL OF MOLECULAR STRUCTURE (2023)

添加到收藏夹

Article Chemistry, Physical

Design, synthesis, and antiproliferative properties of new 1,2,3-triazole-carboximidamide derivatives as dual EGFR/VEGFR-2 inhibitors

Mohamed A. Mahmoud, Anber F. Mohammed, Ola I. A. Salem, Safwat M. Rabea, Bahaa G. M. Youssif

Summary: A new series of substituted aryl carboximidamide VIa-o was designed and synthesised, and their structures were confirmed using spectroscopy and elemental analysis. The antiproliferative effect of these compounds against four cancer cell lines was investigated, and VIc, VIg, VIj, VIk, VIm, and VIo showed the strongest activity. Molecular docking simulations revealed that VIc, VIk, and VIo exhibited high affinity and active site interactions with EGFR and VEGFR-2 enzymes, suggesting their potential as dual inhibitors. Compound VIk demonstrated the highest induced levels of apoptotic markers in A-549 cancer cells, indicating its pro-apoptotic effect. ADME studies showed that the active compounds had good safety and pharmacokinetic profiles.

JOURNAL OF MOLECULAR STRUCTURE (2023)

添加到收藏夹

Article Pharmacology & Pharmacy

Development of Olive Oil Containing Phytosomal Nanocomplex for Improving Skin Delivery of Quercetin: Formulation Design Optimization, In Vitro and Ex Vivo Appraisals

Omnia M. Hendawy, Mohammad M. Al-Sanea, Rehab Mohammed Elbargisy, Hidayat Ur Rahman, Hesham A. M. Gomaa, Ahmed A. B. Mohamed, Mohamed F. Ibrahim, Abdulsalam M. Kassem, Mohammed Elmowafy

Summary: The objective of this study was to fabricate, optimize, and assess olive oil/phytosomal nanocarriers for improved quercetin skin delivery. The optimized formulation, selected using a Box-Behnken design, showed better stability at ambient temperature and higher skin permeation of quercetin compared to the control. The optimized formulation also demonstrated alteration to skin barriers without remarkable toxicity aspects, indicating the potential of olive oil/phytosomal nanocarriers as carriers for quercetin.

PHARMACEUTICS (2023)

添加到收藏夹

Article Chemistry, Medicinal

Design, Synthesis, and Anti-Proliferative Action of Purine/Pteridine-Based Derivatives as Dual Inhibitors of EGFR and BRAFV600E

Samar A. El-Kalyoubi, Hesham A. M. Gomaa, Elshimaa M. N. Abdelhafez, Mohamed Ramadan, Fatimah Agili, Bahaa G. M. Youssif

Summary: The investigation focused on designing and synthesizing purine/pteridine-based derivatives as dual inhibitors of EGFR and BRAF(V600E) for targeted cancer treatment. The majority of the compounds displayed promising antiproliferative activity on cancer cell lines. Compounds 5a, 5e, and 7e of purine-based and pteridine-based scaffolds were identified as the most potent hits, exhibiting strong anti-proliferative and EGFR inhibitory activities. However, the results suggested that BRAF(V600E) may not be a viable target for this class of organic compounds. Molecular docking studies provided insight into possible binding modes at the active sites of EGFR and BRAF(V600E).

PHARMACEUTICALS (2023)

添加到收藏夹

Article Biochemistry & Molecular Biology

Synthesis, Antioxidant and Antiproliferative Actions of 4-(1,2,3-Triazol-1-yl)quinolin-2(1H)-ones as Multi-Target Inhibitors

Essmat M. El-Sheref, Stefan Braese, Hendawy N. Tawfeek, Fatmah Ali Alasmary, Bahaa G. M. Youssif

Summary: The reaction between 4-azido-quinolin-2(1H)-ones and active methylene compounds was studied, leading to the synthesis of a series of 4-(1,2,3-triazol-1-yl)quinolin-2(1H)-ones. Compounds 3f-j showed potent antiproliferative activity and exhibited potential as multi-target inhibitors of EGFR, BRAF(V600E), and EGFR(T790M). Moreover, compounds 3g and 3h demonstrated caspase activation, down-regulation of antiapoptotic Bcl2, and promising antioxidant activity.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2023)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design, Synthesis, and Biological Evaluation of Novel 3-Cyanopyridone/Pyrazoline Hybrids as Potential Apoptotic Antiproliferative Agents Targeting EGFR/BRAFV600E Inhibitory Pathways

Lamya H. Al-Wahaibi, Hesham A. Abou-Zied, Mohamed Hisham, Eman A. M. Beshr, Bahaa G. M. Youssif, Stefan Brase, Alaa M. Hayallah, Mohamed Abdel-Aziz

Summary: A series of novel 3-cyanopyridone/pyrazoline hybrids exhibiting dual inhibition against EGFR and BRAF(V600E) have been developed and demonstrated remarkable antiproliferative activity and promising anticancer potential.

MOLECULES (2023)

添加到收藏夹

Article Biochemistry & Molecular Biology

New 1,2,3-Triazole/1,2,4-triazole Hybrids as Aromatase Inhibitors: Design, Synthesis, and Apoptotic Antiproliferative Activity

Mohamed T-E Maghraby, Tahani Mazyad Almutairi, Stefan Brase, Ola I. A. Salem, Bahaa G. M. Youssif, Mahmoud M. Sheha

Summary: A novel series of 1,2,3-triazole/1,2,4-triazole hybrids were designed and synthesized as antiproliferative agents targeting aromatase enzymes. Compounds 6a and 6b demonstrated the highest antiproliferative activity and aromatase inhibitory action, indicating their potential as anticancer candidates. Molecular docking investigations further supported these findings.

MOLECULES (2023)

添加到收藏夹

Article Biochemistry & Molecular Biology

Discovery of new 5-substituted-indole-2-carboxamides as dual epidermal growth factor receptor (EGFR)/cyclin dependent kinase-2 (CDK2) inhibitors with potent antiproliferative action

Fatma A. M. Mohamed, Saleha Y. M. Alakilli, Eman Fawzy El Azab, Faris A. M. Baawad, Esraa Ibrahim A. Shaaban, Heba Abu Alrub, Omnia Hendawy, Hesham A. M. Gomaa, Adel G. Bakr, Mostafa H. Abdelrahman, Laurent Trembleau, Anber F. Mohammed, Bahaa G. M. Youssif

Summary: A series of 5-substituted-3-ethylindole-2-carboxamides 5a-k and 6a-c were synthesized and investigated for their antiproliferative activity. The compounds showed significant antiproliferative activity against four cancer cell lines, with potent derivatives being compounds 5g, 5i, and 5j. Moreover, compounds 5i and 5j displayed potent antiproliferative activity and can be considered as potential dual EGFR and CDK2 inhibitors.

RSC MEDICINAL CHEMISTRY (2023)

添加到收藏夹

Article Chemistry, Physical

Design and synthesis of new quinoline-ester/-amide derivatives as potent antiproliferative agent targeting EGFR and BRAFV600E kinases

Aliaa M. Mohassab, Heba A. Hassan, Hesham A. Abou-Zied, Mikako Fujita, Masami Otsuka, Hesham A. M. Gomaa, Bahaa G. M. Youssif, Mohamed Abdel-Aziz

Summary: New quinoline-based derivatives were synthesized as promising anti-proliferative candidates. Compound 4a showed the highest inhibitory activity against cancer cell lines and exhibited significant inhibition against EGFR and BRAFV600E. Docking computations suggested compound 4a has favorable affinity towards both EGFR and BRAFV600E.

JOURNAL OF MOLECULAR STRUCTURE (2024)

添加到收藏夹

暂无数据

© Peeref 2019-2024. All rights reserved.