31737-18-5Relevant academic research and scientific papers
Synthesis, Anticancer, and QSAR Studies of 2-Alkyl(aryl,hetaryl)quinazolin-4(3H)-thione's and [1,2,4]Triazolo[1,5-c]quinazoline-2-thione's Thioderivatives
Antypenko, Oleksii M.,Kovalenko, Sergiy I.,Karpenko, Oleksandr V.,Nikitin, Vladyslav O.,Antypenko, Lyudmyla M.
, p. 621 - 631 (2016/08/24)
Considering the frightening high level of mortality from cancer, studies of anticancer agents are vital nowadays. The 24 thioderivatives of 2-alkyl(aryl)-quinazolin-4(3H)-thiones and 20 thioderivatives of [1,2,4]triazolo[1,5-c]quinazoline-2-thiones were synthesized and evaluated for preliminary in?vitro anticancer activity with subsequent in silico QSAR analysis. The substance 18 had the best results inhibiting growth of eight cancer cell lines: CCRF-CEM of leukemia; SF-539, SNB-75, and U251 of CNS cancer; 786, RXF393, and UO-31 of renal cancer; and MDA-MB-231/ATCC of breast cancer (?31.50?–?47.41% of cell growth) with low procancer effect. Calculated QSAR-models for CCRF-CEM of leukemia, T-47D and HS 578T of breast cancer, and mean cell growth demonstrated good rate of anticancer activity prediction (r2?=?0.7?–?0.8, Q2LOO=?0.5?–?0.7).
