Khalil Ashraf A, Abdel-Hamide Sami G, Al-Obaid Abdulrahman M, El-Subbagh Hussein I
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Arch Pharm (Weinheim). 2003 Apr;336(2):95-103. doi: 10.1002/ardp.200390011.
A new series of 2-substituted mercapto-3H-quinozolines bearing 6-iodo and 2-heteroarylthio functions was synthesized and screened for their in vitro antitumor activity. Eighteen compounds were identified as active anticancer agents. N'-[(3-Benzyl-4-oxo-6-iodo-3H-quinazoline-2-yl)thioacetyl]-N(3)-ethylthiosemicarbazide (10), N-benzoyl-N'-[2-(3-benzyl-4-oxo-6-iodo-3H-quinozolin-2-yl)thioacetyl]hydrazine (12), and 2-[(3, 6-dioxo-pyridazin-4-yl)thio]-3-benzyl-4-oxo-6-iodo-3H-quinazoline (20) proved to be the most active members in this study. They showed MG-MID, GI(50) values of 12.8, 11.3, and 13.8 microM, respectively. The detailed synthesis and biological screening data are reported.
合成了一系列带有6-碘和2-杂芳硫基官能团的新型2-取代巯基-3H-喹唑啉,并对其体外抗肿瘤活性进行了筛选。鉴定出18种化合物为活性抗癌剂。N'-[(3-苄基-4-氧代-6-碘-3H-喹唑啉-2-基)硫代乙酰基]-N(3)-乙基硫代氨基脲(10)、N-苯甲酰基-N'-[2-(3-苄基-4-氧代-6-碘-3H-喹唑啉-2-基)硫代乙酰基]肼(12)和2-[(3,6-二氧代哒嗪-4-基)硫代]-3-苄基-4-氧代-6-碘-3H-喹唑啉(20)被证明是本研究中活性最强的成员。它们的MG-MID、GI(50)值分别为12.8、11.3和13.8 microM。报道了详细的合成和生物筛选数据。