Substituted Quinazolines, 1. Synthesis and Antitumor Activity of Certain Substituted 2-Mercapto-4(3H)-quinazolinone Analogs

A new series of 4(3H)-quinazolinone analogs bearing 6-iodo and 2-thioether functions were synthesized and screened for their in vitro antitumor activity. Eight compounds were identified as active anticancer agents. 2-Mercapto-3-benzyl-4-thioxo-6-iodo-3H-quinazolin (2) and 2-(2,4-dinitrophenyl)-3-benzyl-6-iodo-4-(3H)-quinazolinone(9) proved to be the most active compounds in this study. They showed MG-MID GI50, TGI, LC50 values of 3.9, 25.2, 82.3 and 2.7, 12.3, 38.7 μM, respectively. The detailed synthesis and biological screening data are reported

تحضير مشتقات الثيازول واختبارها بيولوجياً كمضادات حيوية ضد الأورام

A series of thiazole derivatives bearing amino, acetamido or thioureido synthons at position 2- and thiosemicarbazone or 1,2,4-triazolethione moieties at position 4- have been synthesized and evaluated for their antimicrobial and antitumor activities. Some of the tested compounds (5,6,14 and 15) proved to possess ^remarkable antitumor antibiotic activity. The antimicrobial potency is found mainly to be against Gram positive bacterfa. The detailed synthesis, spectroscopic and biological data are reported.تم تخليق مجموعة من مشتقات الثيازول واختبارها كمواد لها نشاط ضد البكتريا والأورام . واشتملت هذه المركبات على تلك المشتقات التي تحمل مجاميع أمين أو أسيتاميد أو ثيويوريدو في موقع رقم 2 وكذلك التي تحمل مجاميع ثيوسيميكر بازون أو 4,2,1 - تريازول ثيون في موقع رقم 4 . وقد ثبت أن لبعض المركبات التي تم اختيارها (وهي رقم 5 , 14,6, 15 ) نشاط حيوي قوي وملحوظ ضد الأورام - وقد وجد أن تأثير هدْه المركبات كمضادة للميكروبات يكون أساساً ضد بكتريا جرام الموجبة . وتذكر هذه الدراسة تفاصيل عملية تخليق المركبات ونتائج الدراسات الاسبكتروسكوبية والبيولوجية

Substituted Quinazolines, 1. Synthesis and Antitumor Activity of Certain Substituted 2-Mercapto-4(3H)-quinazolinone Analogs

A new series of 4(3H)-quinazolinone analogs bearing 6-iodo and 2-thioether functions were synthesized and screened for their in vitro antitumor activity. Eight compounds were identified as active anticancer agents. 2-Mercapto-3-benzyl-4-thioxo-6-iodo-3H-quinazolin (2) and 2-(2,4-dinitrophenyl)-3-benzyl-6-iodo-4-(3H)-quinazolinone(9) proved to be the most active compounds in this study. They showed MG-MID GI50, TGI, LC50 values of 3.9, 25.2, 82.3 and 2.7, 12.3, 38.7 μM, respectively. The detailed synthesis and biological screening data are reported.</jats:p

The in vitro antitumor assay of 5-(Z)-arylidene-4-imidazolidinones in screens of AIDS-related leukemia and lymphomas.

Thirty-one different 5-(Z)-arylidene-4-imidazolidinones were tested on six AIDS-related lymphoma (ARL) tumor cell lines, one leukemia CCRF-CEM cell culture and five different lymphoma cell lines: RL, KD-488, AS283, PA682 and SU-DHL-7. The investigated compounds showed remarkable activity against ARL, compounds 3d and 5c proved to inhibit AS283 and SU-DHL-7 cell lines, respectively, both at a GI50 value of 0.03 microM. The 2-(2-carboxyphenylamino) series proved to be the most active members in this investigation. Compounds 6b and 6d showed GI50 (MGMID) values of 6.1 and 8.7 microM, respectively, against the studied six ARL