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Full-Text Articles in Physical Sciences and Mathematics
Synthesis And Antitumor Activities Of 2-(Piperidin-4-Yl)-Thiazole-4-Carboxamides Analogues Of Tubulysins, Xiangfu Peng, Mingsha Shao, Shuchao Ma, Lei Yao
Synthesis And Antitumor Activities Of 2-(Piperidin-4-Yl)-Thiazole-4-Carboxamides Analogues Of Tubulysins, Xiangfu Peng, Mingsha Shao, Shuchao Ma, Lei Yao
Turkish Journal of Chemistry
}Tubulysins are a family of natural products that exhibit potent antitumor activities, which have attracted much attention from synthetic and medicinal chemists. Previous attempts to aromatize the Tuv part of tubulysin analogues led to a loss in antitumor activity, which suggested that the Ile and Tuv fragments of these analogues were adopting different conformations than the natural products. In this study, a series of 2-(piperidin-4-yl)-thiazole-4-carboxamides have been prepared to investigate whether an intramolecular H-bond between key NH and OH groups is responsible for the conformational control. The antitumor activities of these analogues have been screened using MDA-MB-231-breast, Siha-cervical, MCF7-breast, and …
Design, Synthesis, And Antitumor Evaluation Of Novel Methylene Moiety-Tethered Tetrahydroquinoline Derivatives, Esaam Hamied Ahmed Hanashalshahaby, Canan Ünaleroğlu, Ayşe Ak Can, Alp Özgün, Bora Gari̇pcan
Design, Synthesis, And Antitumor Evaluation Of Novel Methylene Moiety-Tethered Tetrahydroquinoline Derivatives, Esaam Hamied Ahmed Hanashalshahaby, Canan Ünaleroğlu, Ayşe Ak Can, Alp Özgün, Bora Gari̇pcan
Turkish Journal of Chemistry
Novel methylene-tethered tetrahydroquinolines (THQs) and cyclopenta[$b$]pyridines were synthesized by one-pot multicomponent reactions of Mannich bases, enolizable ketones, and NH$_{4}$OAc in water by an environmentally friendly K-10 montmorillonite clay-catalyzed reaction. The cytotoxic activities of 1-(2-methyl-8-methylene-5,6,7,8-tetrahydroquinolin-3-yl)ethanone (9a), ethyl 2-methyl-8-methylene-5,6,7,8-tetrahydroquinoline-3 carboxylate (9b), and 1-(2-methyl-7-methylene-6,7-dihydro-5$H$-cyclopenta[$b$]pyridin-3-yl)ethanone (11a) were tested against rat glioblastoma (C6), human breast cancer (MCF-7), prostate cancer (PC3), neuroblastoma (SH-SY5Y), and mouse fibroblast (L929) cell lines in a concentration-dependent (50-300 μM) and time-dependent (24-72 h) manner and expressed as IC$_{50\, }$values. The results showed that compound 9a induced the lowest IC$_{50\, }$values in all cell lines ranging from 111 ± 1.1 μM to …