Synthesis and Cytotoxic Activities of Pyrrole [2,3-d] pyridazin-4-one Derivatives

スポンサーリンク

概要

• 論文の詳細を見る

• 1-Methyl-2-phenyl (1) and 1,3-dimethyl-2-phenyl (2) -substituted pyrrole[2,3-d]pyridazinones, as well as their tetracyclic analogues 3-6, were synthesized and evaluated in vitro by the National Cancer Institute against 60 human tumor cell lines derived from nine cancer cell types. Biological results showed that the antitumor activities of these compounds were related to the planarity of their ring systems with potency increasing in the order 2<4≃5<6<3. Among them, the most potent compound 3 showed significant cell line cytotoxicity, particularly against the renal cancer subpanel [G1_<50> (μM) 5.07] and displayed significant potency [G1_<50> (μM) 3.04-4.32] against MOLT-4, SR (leukemia), NCI-H460 (non-small cell lung), HCT-116 (colon), and SF-295 (CNS) cancer cells, respectively.

• 2002-06-01

著者

• Pinna Gerard

  Dipartimento Farmaco Chimico Tossicologico Universita Di Sassari

• Murineddu Gabriele

  Dipartimento Farmaco Chimico Tossicologico Universita Di Sassari

• Loriga Giovanni

  Dipartimento Farmaco Chimico Tossicologico Universita Di Sassari

• CIGNARELLA Giorgio

  Istituto di Chimica Farmaceutica e Tossicologica, Universita di Milano

• CHELUCCI Giorgio

  Dipartimento di Chimica, Universita di Sassari

• Cignarella Giorgio

  Istituto Di Chimica Farmaceutica E Tossicologica Universita Di Milano

関連論文

• Synthesis and Cytotoxic Activities of Pyrrole [2,3-d] pyridazin-4-one Derivatives
• Synthesis and Anti-HIV-1 Activity of New Delavirdine Analogues Carrying Arylpyrrole Moieties

スポンサーリンク