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 ).

UN SDGs

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

SDG 3 Good Health and Well-being

Keywords

A549 Xenograft
Acute toxicity
Anticancer activity
Pharmacokinetics

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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",

pages = "6633--6636",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd.",

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}

TY - JOUR

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

UR - https://www.scopus.com/pages/publications/77958070232

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

UN SDGs

Keywords

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