Antitumor activity of 3,4-dihydroquinazoline dihydrochloride in A549 xenograft nude mice

Soo Yeon Jung; So Hyung Lee; Han Byul Kang; Hang Ah Park; Sun Ki Chang; Jungahn Kim; Dong Joon Choo; Chun Rim Oh; Young Deuk Kim; Ji Hyung Seo; Kyung Tae Lee; Jae Yeol Lee

doi:10.1016/j.bmcl.2010.09.020

Antitumor activity of 3,4-dihydroquinazoline dihydrochloride in A549 xenograft nude mice

Soo Yeon Jung, So Hyung Lee, Han Byul Kang, Hang Ah Park, Sun Ki Chang, Jungahn Kim, Dong Joon Choo, Chun Rim Oh, Young Deuk Kim, Ji Hyung Seo, Kyung Tae Lee, Jae Yeol Lee

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

35 Citations (Scopus)

Abstract

In the previous article we have reported that 3,4-dihydroquinazoline 1 is a potent and selective T-type calcium channel blocker that exhibited strong anti-cancer activity in vitro. Compound 1·2HCl was further in vivo evaluated against A549 xenograft in BALB/c nude mice, which exhibited 49% tumor-weight inhibition through intravenous administration of 2 mg/kg of body weight and was more potent than doxorubicin. Moreover, compound 1·2HCl has an oral bioavailability of 98% with LD₅₀ values of 693 mg/kg (po route) and 40.0 mg/kg (iv route) of body weight. In addition, its efficient scale-up synthetic method was developed.

Original language	English
Pages (from-to)	6633-6636
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	22
DOIs	https://doi.org/10.1016/j.bmcl.2010.09.020
Publication status	Published - 15 Nov 2010

Bibliographical note

Funding Information:
This research was supported by Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology ( 2010-0028197 ).

Keywords

A549 Xenograft
Acute toxicity
Anticancer activity
Pharmacokinetics

UN SDGs

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

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10.1016/j.bmcl.2010.09.020

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title = "Antitumor activity of 3,4-dihydroquinazoline dihydrochloride in A549 xenograft nude mice",

abstract = "In the previous article we have reported that 3,4-dihydroquinazoline 1 is a potent and selective T-type calcium channel blocker that exhibited strong anti-cancer activity in vitro. Compound 1·2HCl was further in vivo evaluated against A549 xenograft in BALB/c nude mice, which exhibited 49% tumor-weight inhibition through intravenous administration of 2 mg/kg of body weight and was more potent than doxorubicin. Moreover, compound 1·2HCl has an oral bioavailability of 98% with LD50 values of 693 mg/kg (po route) and 40.0 mg/kg (iv route) of body weight. In addition, its efficient scale-up synthetic method was developed.",

keywords = "A549 Xenograft, Acute toxicity, Anticancer activity, Pharmacokinetics",

author = "Jung, {Soo Yeon} and Lee, {So Hyung} and Kang, {Han Byul} and Park, {Hang Ah} and Chang, {Sun Ki} and Jungahn Kim and Choo, {Dong Joon} and Oh, {Chun Rim} and Kim, {Young Deuk} and Seo, {Ji Hyung} and Lee, {Kyung Tae} and Lee, {Jae Yeol}",

note = "Funding Information: This research was supported by Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology ( 2010-0028197 ).",

year = "2010",

month = nov,

day = "15",

doi = "10.1016/j.bmcl.2010.09.020",

language = "English",

volume = "20",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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T1 - Antitumor activity of 3,4-dihydroquinazoline dihydrochloride in A549 xenograft nude mice

AU - Jung, Soo Yeon

AU - Lee, So Hyung

AU - Kang, Han Byul

AU - Park, Hang Ah

AU - Chang, Sun Ki

AU - Kim, Jungahn

AU - Choo, Dong Joon

AU - Oh, Chun Rim

AU - Kim, Young Deuk

AU - Seo, Ji Hyung

AU - Lee, Kyung Tae

AU - Lee, Jae Yeol

N1 - Funding Information: This research was supported by Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology ( 2010-0028197 ).

PY - 2010/11/15

Y1 - 2010/11/15

N2 - In the previous article we have reported that 3,4-dihydroquinazoline 1 is a potent and selective T-type calcium channel blocker that exhibited strong anti-cancer activity in vitro. Compound 1·2HCl was further in vivo evaluated against A549 xenograft in BALB/c nude mice, which exhibited 49% tumor-weight inhibition through intravenous administration of 2 mg/kg of body weight and was more potent than doxorubicin. Moreover, compound 1·2HCl has an oral bioavailability of 98% with LD50 values of 693 mg/kg (po route) and 40.0 mg/kg (iv route) of body weight. In addition, its efficient scale-up synthetic method was developed.

AB - In the previous article we have reported that 3,4-dihydroquinazoline 1 is a potent and selective T-type calcium channel blocker that exhibited strong anti-cancer activity in vitro. Compound 1·2HCl was further in vivo evaluated against A549 xenograft in BALB/c nude mice, which exhibited 49% tumor-weight inhibition through intravenous administration of 2 mg/kg of body weight and was more potent than doxorubicin. Moreover, compound 1·2HCl has an oral bioavailability of 98% with LD50 values of 693 mg/kg (po route) and 40.0 mg/kg (iv route) of body weight. In addition, its efficient scale-up synthetic method was developed.

KW - A549 Xenograft

KW - Acute toxicity

KW - Anticancer activity

KW - Pharmacokinetics

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U2 - 10.1016/j.bmcl.2010.09.020

DO - 10.1016/j.bmcl.2010.09.020

M3 - Article

C2 - 20884207

AN - SCOPUS:77958070232

SN - 0960-894X

VL - 20

SP - 6633

EP - 6636

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 22

ER -

Antitumor activity of 3,4-dihydroquinazoline dihydrochloride in A549 xenograft nude mice

Abstract

Bibliographical note

Keywords

UN SDGs

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