Article
Hematology
Lei Yu, Greggory Myers, Emily Schneider, Yu Wang, Raven Mathews, Kim Chew Lim, David Siemieniak, Vi Tang, David Ginsburg, Ginette Balbin-Cuesta, Sharon A. Singh, Pongpon Phuwakanjana, Natee Jearawiriyapaisarn, Rami Khoriaty, James Douglas Engel
Summary: This study generated a CRISPR knockout library to target erythroid genes and identified novel gamma-globin repressors. Deletion of VHL and PTEN induces HbF synthesis, and small-molecule inhibitors of PTEN and EZH can also induce HbF production.
Article
Chemistry, Multidisciplinary
Fatima Hajizadeh, Mohammad M. Mojtahedi, M. Saeed Abaee
Summary: An efficient metal-free four-component approach for synthesizing piperazine derivatives tethered to an isothiourea group via an ethylene link was developed. The method utilizes in situ generated DABCO salts and involves a two parallel nucleophilic paths to achieve the target products. The protocol exhibited good tolerance towards various DABCO salts and secondary amines, yielding the desired isothiourea-ethylene-tethered-piperazine compounds in high yields.
Article
Chemistry, Medicinal
M. Shaheer Malik, Hissana Ather, Shaik Mohammad Asif Ansari, Ayesha Siddiqua, Qazi Mohammad Sajid Jamal, Ali H. Alharbi, Munirah M. Al-Rooqi, Rabab S. Jassas, Essam M. Hussein, Ziad Moussa, Rami J. Obaid, Saleh A. Ahmed
Summary: Indole-tethered chromene derivatives were efficiently synthesized via a simple reaction using N-alkyl-1H-indole-3-carbaldehydes, 5,5-dimethylcyclohexane-1,3-dione, and malononitrile, catalyzed by DBU at a moderate temperature for a short reaction time, leading to high yields. The synthesized compounds exhibited potent anticancer activity, with compounds 4c and 4d displaying particularly good cytotoxicity against cancer cell lines, and their binding affinity to tubulin protein was superior to the control. Molecular docking and dynamics simulations confirmed the stability of ligand-receptor interactions, and the derivatives passed all drug-likeness filters.
Article
Chemistry, Medicinal
Yuying Fang, Qingyun Tan, Huihao Zhou, Jun Xu, Qiong Gu
Summary: This study discovered a new ferroptosis inducer, FA-S, through phenotypic screenings. Further research showed that FA16, an analog of FA-S, induced ferroptosis by inhibiting system X(-)c. FA16 exhibited better metabolic stability than the classic system X(-)c inhibitor erastin and effectively inhibited tumor growth in vivo.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Yong-Feng Guan, Xiu-Juan Liu, Xin-Ying Yuan, Wen-Bo Liu, Yin-Ru Li, Guang-Xi Yu, Xin-Yi Tian, Yan-Bing Zhang, Jian Song, Wen Li, Sai-Yang Zhang
Summary: In this study, quinoline-chalcone derivatives were designed and synthesized by linking chalcone fragment to the quinoline scaffold, resulting in compound 12e showing promising inhibitory activity against multiple cancer cell lines. Mechanism studies indicated that compound 12e may exert its anticancer effects through various pathways.
Article
Biochemistry & Molecular Biology
Moataz A. Shaldam, Hadia Almahli, Andrea Angeli, Rehab Mustafa Badi, Eman F. Khaleel, Abdelrahman I. Zain-Alabdeen, Zainab M. Elsayed, Eslam B. Elkaeed, Rofaida Salem, Claudiu T. Supuran, Wagdy M. Eldehna, Haytham O. Tawfik
Summary: New isatin-based sulphonamides were synthesized as potential dual VEGFR-2 and carbonic anhydrase inhibitors with anticancer activities. The most potent derivatives showed strong VEGFR-2 inhibitory effect but failed to inhibit relevant CA isoforms. Two derivatives were further tested for their impact on cell cycle disturbance and apoptotic potential. Molecular modelling analyses were conducted to assess the binding mode and stability of the target compounds.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Guangchao Liu, Fuxia Liu, Yue Wang, Xin Liu
Summary: With the increasing global warming, cold stress has become a major factor restricting global crop yield. A novel lncRNA called CIL1 was identified as a positive regulator of the plant response to cold stress in Arabidopsis. CIL1 enhances the plant's resistance to cold stress by regulating the expression of multiple stress-related genes.
Article
Biochemistry & Molecular Biology
Yeongmu Jeong, Sojeong Hong, Hee Jin Jung, Sultan Ullah, YeJi Hwang, Heejeong Choi, Jeongin Ko, Jieun Lee, Pusoon Chun, Hae Young Chung, Hyung Ryong Moon
Summary: This study designed a series of analogs and demonstrated through experiments that analog 2 is an efficient tyrosinase inhibitor that alleviates melanogenesis through dual mechanisms of inhibiting related proteins and genes, as well as directly inhibiting tyrosinase activity.
Article
Chemistry, Medicinal
Omkulthom M. Alkamaly, Najla Altwaijry, Rehab Sabour, Marwa F. Harras
Summary: Novel derivatives of the pyrazoline scaffold showed significant and broad-spectrum anticancer activities with lower cytotoxicity against normal cells. Compounds 5b and 7c were identified as potent dual EGFR and VEGFR2 inhibitors, with strong apoptotic effects on cancer cells. The compounds also demonstrated potential as apoptosis inducers through molecular docking analyses.
ARCHIV DER PHARMAZIE
(2021)
Article
Chemistry, Medicinal
Cangcang Xu, Linfan Xiao, Xia Zhang, Tao Zhuang, Lingli Mu, Xiaoping Yang
Summary: Novel artemisinin ester derivatives were synthesized and compound 2c showed the most potent anti-proliferative activity against OVCAR3 cells with low cytotoxicity, likely through targeting mitochondria and inducing cell apoptosis. These findings suggest compound 2c may be a promising candidate for further investigation against ovarian cancer.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Medicine, Research & Experimental
Dawei Yang, Xiaoyu Tian, Yuchen Ye, Yin Liang, Jie Zhao, Tao Wu, Na Lu
Summary: The study demonstrated that GL-V9 can eliminate senescent cancer cells and induce apoptosis, potentially improving the outcome of cancer chemotherapy.
Article
Biochemistry & Molecular Biology
Ali S. Alqahtani, Mostafa M. Ghorab, Fahd A. Nasr, Mohammad Z. Ahmed, Abdullah A. Al-Mishari, Sabry M. Attia
Summary: In this study, a new series of sulphonamide-bearing quinazolinone derivatives were synthesised and their cytotoxicity in cancer cell lines and normal human cells was evaluated. Compounds 6 and 10 exhibited high anticancer activity and induced cell cycle arrest and apoptosis.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Microbiology
Di Liu, Zhiqin Lun, Ning Liu, Guixin Yuan, Xingbin Wang, Shanshan Li, You-Liang Peng, Xunli Lu
Summary: The fungal pathogen Magnaporthe oryzae secretes a large number of unknown effector proteins that facilitate infection. Through functional screening, we identified four effector genes that induce cell death in rice and one effector gene that induces cell death in Nicotiana benthamiana leaves. Additionally, we found that six effector genes can suppress flg22-induced ROS burst. Further studies showed that the deletion mutants of three effector genes exhibited reduced virulence on rice and barley plants.
Article
Biochemistry & Molecular Biology
Chandrima Gain, Aparna Sarkar, Shrea Bural, Moumita Rakshit, Jeet Banerjee, Ankita Dey, Nabendu Biswas, Gandhi K. Kar, Abhik Saha
Summary: Our study identified two thiophene analogues - compounds 48 and 52, with nearly 4 times greater anti-proliferative efficiency on breast cancer cells compared to natural tanshinones. These compounds induced autophagy-mediated cell death, transcriptionally activated several autophagy genes, and death regulators, supporting their potential as promising leads for further development as anticancer agents by modulating autophagy mechanism.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Physical
Orest Pizio, Stefan Sokolowski
Summary: The wetting phase diagrams for model systems consisting of water and chemically modified graphite surfaces with grafted chain molecules were explored using the density functional approach. The topology of the phase diagram was found to depend on the amount and length of grafted chains.
JOURNAL OF MOLECULAR LIQUIDS
(2022)
