2. Academic Validation
  3. CC-1065 analogues bearing different DNA-binding subunits: synthesis, antitumor activity, and preliminary toxicity study

CC-1065 analogues bearing different DNA-binding subunits: synthesis, antitumor activity, and preliminary toxicity study

  • J Med Chem. 2003 Feb 13;46(4):634-7. doi: 10.1021/jm0203433.
Yuqiang Wang 1,  Lianfa Li,  Wenqing Ye,  Zhiming Tian,  Wei Jiang,  Hong Wang,  Susan C Wright,  James W Larrick
Affiliations

Affiliation

  • 1 Panorama Research, Inc., 2462 Wyandotte Street, Mountain View, California 94043, USA. [email protected]
PMID: 12570384 DOI: 10.1021/jm0203433
Abstract

CC-1065 analogues bearing different DNA-binding subunits were synthesized. A terminal C5-NO2 and -F moiety at the DNA-binding subunit increased the drug's potency and antitumor efficacy. A C5-OCH3 reduced the potency and antitumor efficacy. Compound (+/-)-7, bearing a trans double bond, had increased antitumor efficacy. A preliminary toxicity study indicated that terminal C5-OCH3 and -acetamido moieties at the DNA-binding subunit caused delayed death in mice.

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