Article
Biochemistry & Molecular Biology
Sally Eissa, Amel M. Farrag, Samir Y. Abbas, Mohamed F. El Shehry, Ahmed Ragab, Eman A. Fayed, Yousry A. Ammar
Summary: Designing new biocidal agents by synthesizing hybrid molecules with bioactive moieties is an effective approach. Quinolines with a thiazole moiety showed potent antibacterial and antifungal activities, suggesting them as potential novel agents. Some derivatives demonstrated good peptide deformylase enzyme inhibition activity, indicating their potential as novel bacterial inhibitors.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Sobhi M. Gomha, Hyam A. Abdelhady, Doaa Z. H. Hassain, Aboubakr H. Abdelmonsef, Mohamed El-Naggar, Mahmoud M. Elaasser, Huda K. Mahmoud
Summary: Hybrid drug design is an important method for developing novel anticancer therapies, with thiazole-thiophene hybrids showing promising anticancer activity. The Rab7b protein has been identified as a potential target for novel anticancer agents. In this study, compounds 9 and 11b showed significant antitumor activity against MCF-7 tumor cells, suggesting their potential as lead compounds for new anticancer drugs.
DRUG DESIGN DEVELOPMENT AND THERAPY
(2021)
Article
Chemistry, Multidisciplinary
Alaa M. Alqahtani, Abrar A. Bayazeed
Summary: Ten new pyridine-linked thiazole hybrids were synthesized using a specific strategy, and their cytotoxicity against various cancer cell lines was studied. Two of the compounds showed promising anticancer activity.
ARABIAN JOURNAL OF CHEMISTRY
(2021)
Article
Chemistry, Physical
Molood Naziri, Masoud Mokhtary, Fariba Safa
Summary: Fifteen new substituted quinazoline analogs were successfully synthesized through the reaction of 7-(2-chloroethoxy)-6-methoxy-N-arylquinazoline-4-amine and secondary amines. The cytotoxicity of the synthesized compounds on HU02 and A431 cell lines was evaluated using MTT method. Compound 3f carrying piperidine with 3-chloroaniline showed the highest cytotoxicity, while cytotoxicity against HU02 cells was not favorable. Molecular docking analysis revealed a smaller hydrogen bond distance between quinazoline N1 and the Met-769 residue of EGFR in compound 3f, indicating its greater cytotoxicity.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Biochemistry & Molecular Biology
Gabriel Jasinski, Emir Salas-Sarduy, Daniel Vega, Lucas Fabian, Maria Florencia Martini, Albertina G. Moglioni
Summary: This study evaluated the effects of eleven thiosemicarbazones on cruzipain and investigated their interactions with the enzyme's active site and inhibition mechanism through computational methods. The results suggest that thiosemicarbazones exhibit inhibitory activity against cruzipain.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Organic
Hala F. Rizk, Mohamed A. El-Borai, Ahmed Ragab, Seham A. Ibrahim, Mohamed E. Sadek
Summary: A new series of coloring compounds based on heterocyclic analogues thiazole were synthesized and characterized. These compounds exhibited less toxic and resisted antimicrobial activity, as well as increased antioxidant properties. Additionally, they showed lower cytotoxicity against HepG-2 cells compared to existing compounds.
POLYCYCLIC AROMATIC COMPOUNDS
(2023)
Article
Biochemistry & Molecular Biology
Mohamed A. El-Atawy, Najla A. Alshaye, Nada Elrubi, Ezzat A. Hamed, Alaa Z. Omar
Summary: A variety of structurally different pyrimidines were synthesized and tested for anti-proliferative activity against various cancer cell lines and normal cells. Compounds 3b and 3d showed promising potential for treating prostate cancer, being more potent than the reference drug vinblastine sulfate. Additionally, compounds 3b, 3f, 3g, 3h, and 5 were found to be more selective and safer than vinblastine sulfate, indicating their potential as new cancer treatments.
Article
Multidisciplinary Sciences
Ghadah F. Aljohani, Tariq Z. Abolibda, Mohammad Alhilal, Jehan Y. Al-Humaidi, Suzan Alhilal, Hoda A. Ahmed, Sobhi M. Gomha
Summary: Cancer, one of the deadliest diseases, claims millions of lives annually, prompting the need for novel treatments. In this study, a series of novel thiadiazoles were designed and evaluated for their growth-inhibitory potential against liver cancer cells. Promising anticancer activity was observed in two compounds.
JOURNAL OF TAIBAH UNIVERSITY FOR SCIENCE
(2022)
Article
Chemistry, Medicinal
Shagufta Naz, Fawad Ali Shah, Humaira Nadeenn, Sadia Sarwar, Zhen Tan, Muhammad Imran, Tahir Ali, Jing Bo Li, Shupeng Li
Summary: The study synthesized compounds targeting multiple cellular networks involved in cancer development and identified S3c, S5b, and S6c as promising candidates with anticancer activity in cisplatin-resistant cell lines, suggesting their potential as lead compounds for new anticancer drugs.
DRUG DESIGN DEVELOPMENT AND THERAPY
(2021)
Article
Biochemistry & Molecular Biology
Rabia Basri, Saeed Ullah, Ajmal Khan, Suraj N. Mali, Oussama Abchir, Samir Chtita, Ahmed El-Gokha, Parham Taslimi, Ammena Y. Binsaleh, Attalla F. El-kott, Ahmed Al-Harrasi, Zahid Shafiq
Summary: In this study, the synthesis, alpha-glucosidase inhibition, structure activity relationship, pharmacokinetics, and docking analysis of novel chromone-based thiosemicarbazones were reported. The derivatives exhibited potent activity against alpha-glucosidase, with certain compounds showing higher inhibitory activity than the standard acarbose. Moreover, a statistically significant 2D-QSAR model was developed for further design of potent thiosemicarbazones as alpha-glucosidase inhibitors.
BIOORGANIC CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Rabia Basri, Saeed Ullah, Sobia Ahsan Halim, Rima D. Alharthy, Umair Rauf, Ajmal Khan, Javid Hussain, Ahmed Al-Ghafri, Ahmed Al-Harrasi, Zahid Shafiq
Summary: Inhibiting alpha-glucosidase is an effective method for reducing blood sugar levels in diabetic individuals. Several novel chromen-linked hydrazine carbothioamide compounds were synthesized and screened for their alpha-glucosidase inhibitory potential.
DRUG DEVELOPMENT RESEARCH
(2023)
Article
Biochemistry & Molecular Biology
Rafaqat Hussain, Shahid Iqbal, Mazloom Shah, Wajid Rehman, Shoaib Khan, Liaqat Rasheed, Fazal Rahim, Ayed A. Dera, Sana Kehili, Eslam B. Elkaeed, Nasser S. Awwad, Majed A. Bajaber, Mohammed Issa Alahmdi, Hamad Alrbyawi, Hashem O. Alsaab
Summary: In this study, analogs of benzimidazole containing a thiazole moiety were synthesized and evaluated for their inhibitory activity against alpha-amylase and alpha-glucosidase. The size and hydrogen bonding capability of substituents were found to affect the inhibitory potentials of the analogs.
Article
Chemistry, Medicinal
Said Dadou, Ahmet Altay, Mohammed Koudad, Burcin Turkmenoglu, Esma Yeniceri, Sema Caglar, Mustapha Allali, Adyl Oussaid, Noureddine Benchat, Khalid Karrouchi
Summary: A new series of imidazo[2, 1-b]thiazole-based chalcone derivatives were designed, synthesized, and tested for their anticancer activities. Compound 3j exhibited the best anticancer activity on MCF-7 cells, and further studies revealed its mechanism of action involving mitochondrial membrane depolarization, multicaspase activation, and apoptosis induction.
MEDICINAL CHEMISTRY RESEARCH
(2022)
Article
Agriculture, Multidisciplinary
Meng Li, Weiwei Wang, Xiang Cheng, Yunxiao Wang, Yao Chen, Jiexiu Gong, Xihao Chang, Xianhai Lv
Summary: In this study, a series of pyrazole carboxamide thiazole derivatives were designed, synthesized, and evaluated for their antifungal activities against plant pathogens. The bioassay results showed that several compounds exhibited good antifungal activities, with compounds 6i and 19i showing better efficacy than the control drug. Compound 23i also displayed significant inhibitory activity against a potato pathogen. Scanning electron microscopy analyses revealed that compound 6i could disrupt the surface morphology of the target fungus.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Keyvan Pedrood, Maedeh Sherafati, Maryam Mohammadi-Khanaposhtani, Mohammad Sadegh Asgari, Samanesadat Hosseini, Hossein Rastegar, Bagher Larijani, Mohammad Mahdavi, Parham Taslimi, Yavuz Erden, Sevilay Gunay, Ilhami Gulcin
Summary: Novel quinazolinone derivatives were synthesized and evaluated for their inhibitory activities against various metabolic enzymes, showing high inhibitory activities. The most potent compounds against each enzyme were selected to evaluate their interaction modes in the active site, while cytotoxicity assays demonstrated that these compounds do not exhibit significant cytotoxic effects on cancer cell lines.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
