[BIS(AMINOMETHYL)DIMETHYLSILANE]PLATINUM(II) DICHLORIDE - A POTENTIAL ANTITUMOR AGENT

被引：7

作者：

HAUGWITZ, RD

ANDERSON, WK

PLOWMAN, J

KASLINAL, R

HOUSTON, DM

NARAYANAN, VL

机构：

[1] Division of Cancer Treatment, National Cancer Institute, Bethesda, Maryland

[2] Department of Medicinal Chemistry, School of Pharmacy, State University of New York, Buffalo

来源：

APPLIED ORGANOMETALLIC CHEMISTRY | 1990年 / 4卷 / 04期

关键词：

aminoalkylsilane platinum complex; Antitumor agent; bioisostere; cisplatin;

D O I：

10.1002/aoc.590040410

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

[Bis(aminomethyl)dimethylsilane]platinum(II) dichloride (1) was synthesized by a three‐step procedure. The antitumor activity of 1 was evaluated in the i.p. implanted mouse L1210 leukemia model. A 10 mg kg−1 dose administered every fourth day for a total of three injections extended the median life span of the dying mice by at least 100% and resulted in 40–50% survivors (day 30) in two experiments corresponding to an approximate 6 log10 reduction in tumor burden at the end of treatment. Compound 1 appeared at least as active as cisplatin under the testing protocols utilized. The closely related bis[aminomethyltrimethylsilane]platinum(II) dichloride complex was inactive in this mouse model. Copyright © 1990 John Wiley & Sons Ltd.

引用

页码：375 / 378

页数：4

共 8 条

[1]

Anderson WK, Quagliato DA, Haugwitz RD, Narayanan VL, Wolpert-DePhilippes MK, Cancer Treat. Rep., 70, (1986)

[2]

Rahman A, Roh JK, Wolpert-DePhilippes MK, Goldin A, Vendetti JM, Cancer Res., 48, (1988)

[3]

Smith JH, Smith MA, Litterst C, Copley M, Uozumi, Boyd MR, Pharmacologist, 27, (1985)

[4]

Mathison IW, Solomons WE, Morgan PH, Tidwell RR, Structural Features and Pharmacologic Activity, Principles of Medicinal Chemistry, (1989)

[5]

Geran RI, Greenberg NH, Macdonald MM, Schumacher AM, Abbott BJ, Cancer Chemother. Rep., Part 3, 3, (1972)

[6]

(1976)

[7]

Schabel FM, Griswold DP, Laster WR, Corbett TH, Lloyd HH, Pharmacol Ther., 1, (1977)

[8]

Tacke R, Strecker M, Lambrecht G, Moser U, Mutschler E, Arch Pharm. (Weinheim), 317, (1984)

← 1 →