An Overview on the Development of New Potentially Active Camptothecin Analogs Against Cancer

作者：Chazin Eliza de Lucas; Reis Raisa da Rocha; Vellasco Junior Walcimar Trindade; Elmor Moor Lucas Fajardo; Alves Vasconcelos Thatyana Rocha

来源：Mini Reviews in Medicinal Chemistry, 2014, 14(12): 953-962.

DOI：10.2174/1389557514666141029233037

• Camptothecin
• cancer
• drugs
• homocamptothecin
• irinotecan
• topoisomerase inhibitors
• topotecan

Camptothecin (CPT) and its derivatives comprise an important group of heterocyclic compounds that are well recognized for their anticancer activities. Efforts have been made over the years aiming to develop new CPT analogs with better clinical efficacy, improved pharmacokinetic profile and lower toxicity. First generation of analogs, irinotecan (CPT-11) and topotecan (TPT) was approved for use by FDA in 1996 for the treatment of colorectal (CPT-11) and cervical, ovarian and small lung cancers (TPT). Other analogs of CPT are currently in different phases of clinical trials. As CPT represents an important lead compound in the field of antitumor-research, in this review we will highlight some recent discoveries (2008-2013) on the development of novel camptothecin-based compounds as potential anticancer agents.

• 出版日期2014