670280-44-1Relevant academic research and scientific papers
2-Alkyl(aryl)-quinazolin-4(3 H)-thiones, 2-R-(quinazolin-4(3 H)-ylthio)carboxylic acids and amides: Synthesis, molecular docking, antimicrobial and anticancer properties
Antypenko, Lyudmyla,Kovalenko, Sergiy,Posylkina, Yulia,Nikitin, Vladyslav,Fedyunina, Natalia,Ivchuk, Vitalii
, p. 253 - 265 (2016/02/03)
In this study, a series of novel 2-alkyl(aryl)-quinazolin-4(3H)-thiones, 2-R-(quinazolin-4(3H)-ylthio)carboxylic acids and amides were synthesized and evaluated for antimicrobial and anticancer activities. Their structure was confirmed by elemental analys
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).
Studies on quinazolines. Part III. Synthesis of some fused-ring cationic and mesoionic derivatives of the 1,3-thiazolo[3,2-c]quinazoline ring system
Wasfy
, p. 1901 - 1910 (2007/10/03)
4-Allylthio-2-arylquinazolines 4a-c undergo cyclization by action of bromine to furnish 5-aryl-3-bromomethyl-2,3-dihydrothiazolo[3,2-c]quinazolin-4- ium bromide 5a-c. Compounds 5a-c undergo ring opening by action of water under acid catalysis to afford th
Cationic and mesoionic 1,3-thiazolo-[3,2-c]quinazoline derivatives
Wasfy
, p. 576 - 580 (2007/10/03)
4-Allylthio-2-arylquinazolines 4a-c undergo cyclization by action of bromine to furnish 5-aryl-3-bromomethyl-2,3-dihydrothiazolo[3,2-c]quinazolin-4-ium bromides 5a-c. Compounds 5a-c undergo ring opening by action of water under acid catalysis to afford the corresponding dibromide derivatives 6a-c. Bromination of 3-allyl-2-aryl-4(3H)quinazolinethiones 7a-c leads to 5-aryl-2-bromomethyl-2,3-dihydrothiazolo[3,2-c]quinazolin-4-ium bromides 8a-c. However, anhydro-3-hydroxy-5-aryl-1,3-thiazolo[3,2-c]quinazolin-4-ium hydroxide 10a-c were prepared by the cyclodehydration of the corresponding thioglycolic acids 9a-c with Ac2O.
