Article
Chemistry, Medicinal
Chao Liu, Yuan-Yuan Xu, Zhao-Hui Wen, Yue-Hui Dong, Zhao-Peng Liu
Summary: The study reported the synthesis and evaluation of antitumor activity of two series of BU-4664L derivatives. All derivatives displayed micromolar activity against PC-3 cells, with 10a and 16c showing the most promising antiproliferative activity.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2022)
Article
Chemistry, Medicinal
Sung-Bau Lee, Ting-Yu Chang, Nian-Zhe Lee, Zih-Yao Yu, Chi-Yuan Liu, Hsueh-Yun Lee
Summary: This study introduces novel bisindole molecules as anti-cancer agents that effectively inhibit TLKs activity and demonstrated their anti-cancer effects in vitro. Through structure optimization, six derivatives with potent TLK inhibitory activity were identified, with potential applications in the treatment of various cancers.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Valeria Stefanizzi, Antonella Minutolo, Elena Valletta, Martina Carlini, Franca M. M. Cordero, Anna Ranzenigo, Salvatore Pasquale Prete, Daniel Oscar Cicero, Erica Pitti, Greta Petrella, Claudia Matteucci, Francesca Marino-Merlo, Antonio Mastino, Beatrice Macchi
Summary: Metal-derived platinum complexes are commonly used in the treatment of solid tumors. However, the toxicity and resistance of these drugs necessitate the search for alternative compounds. Organotin compounds have shown potential in inhibiting cell growth and inducing cell death and autophagy. In this study, the biological activities of different organotin compounds were evaluated, and it was found that tributyltin compounds were more cytotoxic than cisplatin. Additionally, the mechanism of action was attributed to the inhibition of glucose uptake. Furthermore, the tumorigenicity of the cells influenced their susceptibility to the compounds, with highly tumorigenic cells being less affected.
Article
Biochemistry & Molecular Biology
Yichang Ren, Yong Ruan, Binbin Cheng, Ling Li, Jin Liu, Yuyu Fang, Jianjun Chen
Summary: Compound 3b, designed as a tubulin inhibitor targeting the colchicine binding site, showed high antiproliferative activity against HepG-2 cells, with the ability to suppress microtubule polymerization, disrupt dynamics, inhibit cancer cell migration, induce cell cycle arrest and apoptosis. Docking studies indicated its potential as a novel tubulin inhibitor deserving further investigation.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Leila Emami, Soghra Khabnadideh, Zahra Faghih, Farnoosh Farahvasi, Fatemeh Zonobi, Saman Zare Gheshlaghi, Shadi Daili, Ali Ebrahimi, Zeinab Faghih
Summary: A series of quinazolinone derivatives were synthesized as antiproliferative agents and evaluated for their structure and cytotoxic activity. Molecular docking studies confirmed their potential anticancer activity and most of the compounds fulfilled drug design rules. With further modification, these compounds could be promising antiproliferative agents.
Article
Biochemistry & Molecular Biology
Jing Li, Ru Si, Qingqing Zhang, Yanchen Li, Jie Zhang, Yuanyuan Shan
Summary: Based on the scaffold hybridization strategy, twenty-four indole-guanidines were designed and synthesized. Most of these hybrids exhibited moderate to high anti-proliferative activity against various cancer cells, especially human hepatoma cell lines. Selectivity investigation showed that the hybrids had the best selectivity for the SMMC-7721 subtype in human hepatoma cells. Particularly, compound 22 demonstrated potent inhibition against SMMC-7721 cells, inducing apoptosis and cell cycle arrest in a dose-dependent manner, while down-regulating the expression of specific proteins.
CHEMICO-BIOLOGICAL INTERACTIONS
(2022)
Article
Chemistry, Multidisciplinary
Aya Y. Hemaida, Ghada S. Hassan, Azza R. Maarouf, Jacques Joubert, Ali A. El-Emam
Summary: Nineteen new thiazole-based derivatives were synthesized and compounds 10 and 16 showed potent AChE inhibitory activities, making them potential lead compounds for the development of new and improved AChE inhibitors.
Article
Biochemistry & Molecular Biology
Wu-Xi Zhou, Chen Chen, Xiao-Qin Liu, Ying Li, Ling-Yi Kong, Jian-Guang Luo
Summary: Novel derivatives of withangulatin A (WA) were synthesized and evaluated for their antiproliferative activity against four human cancer cell lines, with compound 10 showing the most potent activity against the human breast cancer cell line MDA-MB-231. Compound 10 also demonstrated a high selectivity index for breast cancer MDA-MB-231 cells, indicating its potential as a promising anticancer agent.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Serdar Burmaoglu, Arzu Gobek, Busra Ozturk Aydin, Emine Yurtoglu, Busra Nur Aydin, Gozde Yalcin Ozkat, Ceylan Hepokur, Nihal Simsek Ozek, Ferhunde Aysin, Ramazan Altundas, Oztekin Algul
Summary: Building on previous work on chalcone as a pharmacophore for anticancer activity, the study synthesized novel bischalcones and found compound 6c to exhibit the highest antiproliferative activity, induce cell cycle arrest, and have a high apoptosis/necrosis ratio. Molecular docking studies supported its anticancer properties, suggesting its potential for lung cancer treatment.
BIOORGANIC CHEMISTRY
(2021)
Article
Engineering, Chemical
Aneta Baj, Lucie Rarova, Artur Ratkiewicz, Miroslav Strnad, Stanislaw Witkowski
Summary: a-TS and a-TEA are effective compounds for inducing apoptosis in cancer cells and suppressing tumor growth, while showing limited or no toxicity towards nonmalignant cells. The introduction of an alkyl substituent in a-TEA increased its anticancer activity, with a-Tocopheryloxy-2-methylpropanoic acid being more active and non-toxic to normal cells. Molecular docking study further supported the biological activity of the synthesized compounds. This research confirmed the potential therapeutic use of vitamin E derivatives as anticancer agents.
Article
Chemistry, Medicinal
Bilgesu Onur Sucu
Summary: In this study, two series of imidazopyridine derivatives were synthesized and evaluated for their antiproliferative potential in breast cancer cells. The pyrimidine-containing compounds did not show activity, while the N-acylhydrazone derivatives exhibited significant activity. Compound 15 showed the most potent activity against the MCF7 and MDA-MB-231 cell lines.
MEDICINAL CHEMISTRY RESEARCH
(2022)
Article
Biochemistry & Molecular Biology
Valentina Noemi Madia, Alice Nicolai, Antonella Messore, Alessandro De Leo, Davide Ialongo, Valeria Tudino, Francesco Saccoliti, Daniela De Vita, Luigi Scipione, Marco Artico, Samanta Taurone, Ludovica Taglieri, Roberto Di Santo, Susanna Scarpa, Roberta Costi
Summary: The study designed and evaluated a series of new aminopyrimidine derivatives structurally related to RDS 3442 for their ability to inhibit cell proliferation on various tumor cell lines. The N-benzyl counterpart 2a showed significant decrease in cell viability in all tested tumor cell lines, with EC(50)s ranging from 4 to 8 mu M, 4-13 times more active than the hit compound.
Article
Biochemistry & Molecular Biology
Beata Tylinska, Benita Wiatrak, Zaneta Czyznikowska, Aneta Ciesla-Niechwiadowicz, Elzbieta Gebarowska, Anna Janicka-Klos
Summary: New pyrimidine derivatives were designed, synthesized, and analyzed for their anticancer properties in this study. The compounds exhibited inhibitory activity on various cancer cell lines, with stronger impact on P-glycoprotein activity in doxorubicin-resistant cell cultures. These compounds showed more lipophilic character than doxorubicin, determining their affinity for molecular targets and passive transport through biological membranes. Additionally, their potential as inhibitors of topoisomerase II and DNA intercalation was investigated through molecular docking.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Medicinal
Xiaojing Sun, Lin Xing, Jieying Yuan, Enxiao Wang, Yuxin Ding, Ruilong Sheng, Fang Wang, Wenhui Wu, Xiuwei H. Yang, Ruihua Guo
Summary: In this study, a new series of DEM derivatives were synthesized by modifying active groups in the chemical structure of DEM. Among them, derivative 7 showed remarkable inhibitory effect on three human cancer cell lines (A549, HCT116, and HeLa) and induced apoptosis in tumor cells.
Article
Chemistry, Multidisciplinary
Mahmoud A. Alelaimat, Mahmoud A. Al-Sha'er, Haneen A. Basheer
Summary: Trisubstituted 1,3,5-triazine derivatives have biological benefits in reducing inflammation and fighting cancer. A series of unique sulfonamide-triazine hybrid molecules were synthesized using the solvent-free/neat fusion method, and their novel structures were identified through spectroscopic analyses. Promising anticancer activity was observed in compound 34, which showed high inhibition against the PI3K alpha enzyme and potential for developing targeted anticancer compounds.
