New imidazo[2,1-b]thiazole derivatives: Synthesis, in vitro anticancer evaluation, and in silico studies

Jin Hun Park; Mohammed I. El-Gamal; Yong Sup Lee; Chang Hyun Oh

doi:10.1016/j.ejmech.2011.08.024

New imidazo[2,1-b]thiazole derivatives: Synthesis, in vitro anticancer evaluation, and in silico studies

Jin Hun Park, Mohammed I. El-Gamal, Yong Sup Lee, Chang Hyun Oh

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

98 Citations (Scopus)

Abstract

A series of 18 new imidazo[2,1-b]thiazole derivatives was synthesized. Their in vitro antiproliferative activities against A375P human melanoma cell line and NCI-60 cell line panel were tested. Compounds 15, 16, 18, 22, 26-28, and 31 showed superior potency against A375P to sorafenib. In addition, compounds 26 and 27 showed selectivity toward melanoma cell lines than for other cancer types. Both compounds exerted sub-micromolar IC₅₀ values over 7 (including A375P) and 6 melanoma cell lines, respectively. In silico studies are also reported. ADME profiling, in silico toxicity, drug-likeness, and drug-score data of compounds 26 and 27 are promising.

Original language	English
Pages (from-to)	5769-5777
Number of pages	9
Journal	European Journal of Medicinal Chemistry
Volume	46
Issue number	12
DOIs	https://doi.org/10.1016/j.ejmech.2011.08.024
Publication status	Published - Dec 2011

Bibliographical note

Funding Information:
We are grateful to the National Cancer Institute (NCI), Bethesda, Maryland, USA, for performing the anticancer testing over the 60-cancer cell line panel. We would like to thank Korea Institute of Science and Technology (KIST) for financial support.

Keywords

A375P
Anticancer
Antiproliferative activity
Imidazo[2,1-b]thiazole
Melanoma

UN SDGs

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

Access to Document

10.1016/j.ejmech.2011.08.024

Cite this

@article{d395fb9fb42f4b14973189a0b752f241,

title = "New imidazo[2,1-b]thiazole derivatives: Synthesis, in vitro anticancer evaluation, and in silico studies",

abstract = "A series of 18 new imidazo[2,1-b]thiazole derivatives was synthesized. Their in vitro antiproliferative activities against A375P human melanoma cell line and NCI-60 cell line panel were tested. Compounds 15, 16, 18, 22, 26-28, and 31 showed superior potency against A375P to sorafenib. In addition, compounds 26 and 27 showed selectivity toward melanoma cell lines than for other cancer types. Both compounds exerted sub-micromolar IC50 values over 7 (including A375P) and 6 melanoma cell lines, respectively. In silico studies are also reported. ADME profiling, in silico toxicity, drug-likeness, and drug-score data of compounds 26 and 27 are promising.",

keywords = "A375P, Anticancer, Antiproliferative activity, Imidazo[2,1-b]thiazole, Melanoma",

author = "Park, {Jin Hun} and El-Gamal, {Mohammed I.} and Lee, {Yong Sup} and Oh, {Chang Hyun}",

note = "Funding Information: We are grateful to the National Cancer Institute (NCI), Bethesda, Maryland, USA, for performing the anticancer testing over the 60-cancer cell line panel. We would like to thank Korea Institute of Science and Technology (KIST) for financial support. ",

year = "2011",

month = dec,

doi = "10.1016/j.ejmech.2011.08.024",

language = "English",

volume = "46",

pages = "5769--5777",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson s.r.l.",

number = "12",

}

TY - JOUR

T1 - New imidazo[2,1-b]thiazole derivatives

T2 - Synthesis, in vitro anticancer evaluation, and in silico studies

AU - Park, Jin Hun

AU - El-Gamal, Mohammed I.

AU - Lee, Yong Sup

AU - Oh, Chang Hyun

N1 - Funding Information: We are grateful to the National Cancer Institute (NCI), Bethesda, Maryland, USA, for performing the anticancer testing over the 60-cancer cell line panel. We would like to thank Korea Institute of Science and Technology (KIST) for financial support.

PY - 2011/12

Y1 - 2011/12

N2 - A series of 18 new imidazo[2,1-b]thiazole derivatives was synthesized. Their in vitro antiproliferative activities against A375P human melanoma cell line and NCI-60 cell line panel were tested. Compounds 15, 16, 18, 22, 26-28, and 31 showed superior potency against A375P to sorafenib. In addition, compounds 26 and 27 showed selectivity toward melanoma cell lines than for other cancer types. Both compounds exerted sub-micromolar IC50 values over 7 (including A375P) and 6 melanoma cell lines, respectively. In silico studies are also reported. ADME profiling, in silico toxicity, drug-likeness, and drug-score data of compounds 26 and 27 are promising.

AB - A series of 18 new imidazo[2,1-b]thiazole derivatives was synthesized. Their in vitro antiproliferative activities against A375P human melanoma cell line and NCI-60 cell line panel were tested. Compounds 15, 16, 18, 22, 26-28, and 31 showed superior potency against A375P to sorafenib. In addition, compounds 26 and 27 showed selectivity toward melanoma cell lines than for other cancer types. Both compounds exerted sub-micromolar IC50 values over 7 (including A375P) and 6 melanoma cell lines, respectively. In silico studies are also reported. ADME profiling, in silico toxicity, drug-likeness, and drug-score data of compounds 26 and 27 are promising.

KW - A375P

KW - Anticancer

KW - Antiproliferative activity

KW - Imidazo[2,1-b]thiazole

KW - Melanoma

UR - http://www.scopus.com/inward/record.url?scp=80955151670&partnerID=8YFLogxK

U2 - 10.1016/j.ejmech.2011.08.024

DO - 10.1016/j.ejmech.2011.08.024

M3 - Article

C2 - 22033063

AN - SCOPUS:80955151670

SN - 0223-5234

VL - 46

SP - 5769

EP - 5777

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

IS - 12

ER -

New imidazo[2,1-b]thiazole derivatives: Synthesis, in vitro anticancer evaluation, and in silico studies

Abstract

Bibliographical note

Keywords

UN SDGs

Access to Document

Other files and links

Fingerprint

Cite this