6746-11-8Relevant academic research and scientific papers
Improving the Potency of Cancer Immunotherapy by Dual Targeting of IDO1 and DNA
Fang, Kun,Dong, Guoqiang,Wang, Hongyu,He, Shipeng,Wu, Shanchao,Wang, Wei,Sheng, Chunquan
, p. 30 - 36 (2017/12/26)
Herein we report the first exploration of a dual-targeting drug design strategy to improve the efficacy of small-molecule cancer immunotherapy. New hybrids of indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors and DNA alkylating nitrogen mustards that respectively target IDO1 and DNA were rationally designed. As the first-in-class examples of such molecules, they were found to exhibit significantly enhanced anticancer activity in vitro and in vivo with low toxicity. This proof-of-concept study has established a critical step toward the development of a novel and effective immunotherapy for the treatment of cancers.
Coronarin D conjugated to methylene homologues of chlorambucil: Synthesis and evaluation of their cytotoxicity
Khunnawutmanotham, Nisachon,Chimnoi, Nitirat,Champathong, Wattanachai,Lerdsirisuk, Pradit,Khotmor, Theeraphon,Techasakul, Supanna
experimental part, p. 374 - 378 (2012/10/08)
Methylene homologues of chlorambucil were synthesised and conjugated to the labdane diterpene coronarin D. The products were evaluated for their in vitro cytotoxicity, and were found to exhibit selective activity against MOLT-3 cell line. Two homologues o
DNA-targeted alkylating agents
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, (2008/06/13)
The invention relates to novel bis-benzimidazole compounds which have the ability to bind to the minor groove of DNA and to alkylate DNA, to methods of preparing the compounds, and the use of the compounds in the treatement of neoplastic disease.
Benzimidazole derivatives
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, (2008/06/13)
Disclosed are compounds represented by the following chemical formula (I) and pharmacologically acceptable salts thereof which are novel compounds useful as anticancer agents, antiviral agents or antimicrobial agents. STR1
