Lead optimization of HMBA to develop potent HEXIM1 inducers

Bo Zhong; Rati Lama; Wannarasmi Ketchart; Monica M. Montano; Bin Su

doi:10.1016/j.bmcl.2014.01.025

Lead optimization of HMBA to develop potent HEXIM1 inducers

Bo Zhong
, Rati Lama
, Wannarasmi Ketchart
, Monica M. Montano
, Bin Su

Research output: Contribution to journal › Article › peer-review

5 Scopus citations

Abstract

The potency of a series of Hexamethylene bis-acetamide (HMBA) derivatives inducing Hexamethylene bis-acetamide inducible protein 1 (HEXIM1) was determined in LNCaP prostate cancer cells. Several compounds with unsymmetrical structures showed significantly improved activity. Distinct from HMBA, these analogs have increased hydrophobicity and can improve the short half-life of HMBA, which is one of the factors that have limited the application of HMBA in clinics. The unsymmetrical scaffolds of the new analogs provide the basis for further lead optimization of the compounds using combinatorial chemistry strategy. © 2014 Elsevier Ltd. All rights reserved.

Original language	English
Pages (from-to)	1410-1413
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	24
Issue number	5
DOIs	https://doi.org/10.1016/j.bmcl.2014.01.025
State	Published - Mar 1 2014

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Derivatives
Drug development
HEXIM1
HMBA

Access to Document

10.1016/j.bmcl.2014.01.025

Cite this

@article{6892d6dffef74d0ba19f07da3a434b2f,

title = "Lead optimization of HMBA to develop potent HEXIM1 inducers",

abstract = "The potency of a series of Hexamethylene bis-acetamide (HMBA) derivatives inducing Hexamethylene bis-acetamide inducible protein 1 (HEXIM1) was determined in LNCaP prostate cancer cells. Several compounds with unsymmetrical structures showed significantly improved activity. Distinct from HMBA, these analogs have increased hydrophobicity and can improve the short half-life of HMBA, which is one of the factors that have limited the application of HMBA in clinics. The unsymmetrical scaffolds of the new analogs provide the basis for further lead optimization of the compounds using combinatorial chemistry strategy. {\textcopyright} 2014 Elsevier Ltd. All rights reserved.",

keywords = "Derivatives, Drug development, HEXIM1, HMBA",

author = "Bo Zhong and Rati Lama and Wannarasmi Ketchart and Montano, \{Monica M.\} and Bin Su",

year = "2014",

month = mar,

day = "1",

doi = "10.1016/j.bmcl.2014.01.025",

language = "English",

volume = "24",

pages = "1410--1413",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd",

number = "5",

}

TY - JOUR

T1 - Lead optimization of HMBA to develop potent HEXIM1 inducers

AU - Zhong, Bo

AU - Lama, Rati

AU - Ketchart, Wannarasmi

AU - Montano, Monica M.

AU - Su, Bin

PY - 2014/3/1

Y1 - 2014/3/1

N2 - The potency of a series of Hexamethylene bis-acetamide (HMBA) derivatives inducing Hexamethylene bis-acetamide inducible protein 1 (HEXIM1) was determined in LNCaP prostate cancer cells. Several compounds with unsymmetrical structures showed significantly improved activity. Distinct from HMBA, these analogs have increased hydrophobicity and can improve the short half-life of HMBA, which is one of the factors that have limited the application of HMBA in clinics. The unsymmetrical scaffolds of the new analogs provide the basis for further lead optimization of the compounds using combinatorial chemistry strategy. © 2014 Elsevier Ltd. All rights reserved.

AB - The potency of a series of Hexamethylene bis-acetamide (HMBA) derivatives inducing Hexamethylene bis-acetamide inducible protein 1 (HEXIM1) was determined in LNCaP prostate cancer cells. Several compounds with unsymmetrical structures showed significantly improved activity. Distinct from HMBA, these analogs have increased hydrophobicity and can improve the short half-life of HMBA, which is one of the factors that have limited the application of HMBA in clinics. The unsymmetrical scaffolds of the new analogs provide the basis for further lead optimization of the compounds using combinatorial chemistry strategy. © 2014 Elsevier Ltd. All rights reserved.

KW - Derivatives

KW - Drug development

KW - HEXIM1

KW - HMBA

UR - https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=84894541407&origin=inward

UR - https://www.scopus.com/inward/citedby.uri?partnerID=HzOxMe3b&scp=84894541407&origin=inward

U2 - 10.1016/j.bmcl.2014.01.025

DO - 10.1016/j.bmcl.2014.01.025

M3 - Article

C2 - 24503105

SN - 0960-894X

VL - 24

SP - 1410

EP - 1413

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 5

ER -

Lead optimization of HMBA to develop potent HEXIM1 inducers

Abstract

UN SDGs

Keywords

Access to Document

Other files and links

Cite this