A new chalcone derivative (E)-3-(4-methoxyphenyl)-2-methyl-1-(3,4,5- trimethoxyphenyl)prop-2-en-1-one Suppresses prostate cancer involving p53-mediated cell cycle arrests and apoptosis

Yong Zhang, Balasubramanian Srinivasan, Chengguo Xing, Junxuan Lu

Research output: Contribution to journalArticle

14 Citations (Scopus)

Abstract

Previous studies suggested chalcones as antineoplastic drug candidates. We synthesized a new chalcone derivative (E)-3-(4-methoxyphenyl)-2-methyl-1-(3,4,5- trimethoxyphenyl)prop-2-en-1-one, (CHO27) with an up to 1000-fold increased cytotoxic potency relative to its parent compound in cell culture assays. CHO27 at low nanomolar levels, inhibited prostate cancer (PCa) cell growth through cell cycle arrest and caspase-dependent apoptosis. Activation of p53 accounted for, at least in part, the growth inhibition by CHO27 in vitro. Furthermore, i.p. administration of CHO27 suppressed the growth of established PCa 22Rv1 xenograft tumors accompanied with p53 and p21Cip1 induction. CHO27 may be a lead for development of new therapeutic agents for PCa.

Original languageEnglish (US)
Pages (from-to)3689-3698
Number of pages10
JournalAnticancer Research
Volume32
Issue number9
StatePublished - Sep 1 2012

Fingerprint

Chalcone
Cell Cycle Checkpoints
Prostatic Neoplasms
Apoptosis
Growth
Chalcones
Caspases
Heterografts
Antineoplastic Agents
Cell Culture Techniques
Neoplasms
Therapeutics

All Science Journal Classification (ASJC) codes

  • Oncology
  • Cancer Research

Cite this

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abstract = "Previous studies suggested chalcones as antineoplastic drug candidates. We synthesized a new chalcone derivative (E)-3-(4-methoxyphenyl)-2-methyl-1-(3,4,5- trimethoxyphenyl)prop-2-en-1-one, (CHO27) with an up to 1000-fold increased cytotoxic potency relative to its parent compound in cell culture assays. CHO27 at low nanomolar levels, inhibited prostate cancer (PCa) cell growth through cell cycle arrest and caspase-dependent apoptosis. Activation of p53 accounted for, at least in part, the growth inhibition by CHO27 in vitro. Furthermore, i.p. administration of CHO27 suppressed the growth of established PCa 22Rv1 xenograft tumors accompanied with p53 and p21Cip1 induction. CHO27 may be a lead for development of new therapeutic agents for PCa.",
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A new chalcone derivative (E)-3-(4-methoxyphenyl)-2-methyl-1-(3,4,5- trimethoxyphenyl)prop-2-en-1-one Suppresses prostate cancer involving p53-mediated cell cycle arrests and apoptosis. / Zhang, Yong; Srinivasan, Balasubramanian; Xing, Chengguo; Lu, Junxuan.

In: Anticancer Research, Vol. 32, No. 9, 01.09.2012, p. 3689-3698.

Research output: Contribution to journalArticle

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