synthesis and reactions of some new heterocyclic carbohydrazides and related compounds as potential anticancer agents一些新的杂环的合成和反应carbohydrazides和相关化合物作为潜在的抗癌药物.pdf

Molecules 2003, 8, 744-755 molecules ISSN 1420-3049 / Synthesis and Reactions of Some New Heterocyclic Carbohydrazides and Related Compounds as Potential Anticancer Agents Abdel Kader Mansour *,1, Mohga M. Eid 1 and Nasser S. A. M. Khalil 2 1 Department of Chemistry, Faculty of Science, Cairo University, Giza, Egypt. 2 Central Laboratory for Food and Feed, Agricultural Research Centre, 9 El Gamaa St., Giza, Egypt. *Author to whom correspondence should be addressed; e-mail: nasserkhalil_23@ Received: 1 June 2003; in revised form: 20 August 2003/ Accepted: 25 August 2003 / Published: 31 October 2003 Abstract: Acylation of 3-hydrazino-5,6-diphenyl-1,2,4-triazine (2) and hydrazine hydrate (7) with 4-aryl-1,3,7-triphenyl-8-oxa-1,2,6-triazaspiro[4.4]nona-2,6-dien-9-ones 5a,b gave the corresponding heterocyclic carbohydrazides 6a,b and 8a,b respectively. Conversion of compounds 8a,b into the versatile carbohydrazide derivatives 9a-g, 10, 13 and the related oxadiazoles 11, 12a,b was undertaken. A primary in vitro test of compound 8a (concentration 10-4 M) showed activity against leukemia cell lines (CCRF- CEM, K-256, MOLT-4, PRMI-8226, SR). Keywords: Synthesis, Pyrazoles, 2-Pyrazolines, Carbohydrazides. Introduction Hydrazides and related compounds have been described as useful building blocks for the assembly of various heterocyclic rings [1]. A large number of aliphatic, alicyclic, aromatic and heterocyclic carbohydrazides, their derivatives and related compounds are reported to present a plethora of biological ac