title: Synthesis and antitumor activity of 10-arylcamptothecin derivatives.
abstract: A series of 10-arylcamptothecin derivatives was designed and synthesized. The key step of the synthesis was achieved by employing Suzuki cross-coupling chemistry. All of the new derivatives were tested for cytotoxicity against three human tumor cell lines, BEL-7402, A549, and HL-60; most of the derivatives exhibited potent cytotoxicity. The stability study showed that compound 30 was more stable than its lead compound 10-hydroxycamptothecin under the physiological condition. Mechanistic study demonstrated that compound 30 and its hydrochloride 31 had a pharmacological profile similar with camptothecin.
authors.affiliation: Department of Medicinal Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, PR China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Jiao
authors.forename: Hongchun
authors.initials: H
authors.lastname: Liu
authors.forename: Meiyu
authors.initials: M
authors.lastname: Geng
authors.forename: Wenhu
authors.initials: W
authors.lastname: Duan
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002166:Camptothecin / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006801:Humans; D012995:Solubility
chemical_list: D000970:Antineoplastic Agents; D002166:Camptothecin