Synthesis and Evaluation of Analogues of 5'-([(Z)-4-Amino-2-butenyl]methylamino)-5'-deoxyadenosine as Inhibitors of Tumor Cell Growth, Trypanosomal Growth, and HIV-1 Infectivity

Canio J. Marasco Jr.; Debora L. Kramer; Carl W. Porter; Cyrus J. Bacchi; Donna Rattendi; Louis Kucera; Nathan Iyer; Ralph Bernacki; Paula Pera; Janice R. Sufrin

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Synthesis and Evaluation of Analogues of 5'-([(Z)-4-Amino-2-butenyl]methylamino)-5'-deoxyadenosine as Inhibitors of Tumor Cell Growth, Trypanosomal Growth, and HIV-1 Infectivity

机译：5'-（[（（Z）-4-氨基-2-丁烯基]甲基氨基）-5'-脱氧腺苷作为肿瘤细胞生长，锥虫生长和HIV-1感染抑制剂的合成和评价

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A well-defined series of 5'-([(Z)-4-amino-2-butenyl]methylamino)-5'-deoxyadenosine analogues was designed and synthesized in order to further ascertain the optimal structural requirements for S-adenosylmethionine decarboxylase inhibition and potentially to augment and perhaps separate their antiproliferative and antitrypanosomal activities. Most structural modifications had a deleterious affect on both the antitrypanosmal and antineoplastic activity of 5'-([(Z)-4-amino-2-butenyl]methylamino)-5'-deoxyadenosine. However, di-O-acetylation of the parent compound produced a potential prodrug that caused markedly pronounced inhibition of trypanosomal and neoplastic cell growth and viability. Moreover, the acetylated derivative of 5'-([(Z)-4-amino-2-butenyl]methylamino)-5'-deoxyadenosine did inhibit HIV-1 growth and infectivity, whereas the parent compound did not.

机译：设计并合成了一系列明确定义的5'-（[（（Z）-4-氨基-2-丁烯基]甲基氨基）-5'-脱氧腺苷类似物，以进一步确定抑制S-腺苷甲硫氨酸脱羧酶的最佳结构要求并有可能增强甚至分离它们的抗增殖和抗锥虫活性。大多数结构修饰对5'-（[（（Z）-4-氨基-2-丁烯基]甲基氨基）-5'-脱氧腺苷的抗锥虫活性和抗肿瘤活性均具有有害影响。但是，母体化合物的二-O-乙酰化作用会产生潜在的前药，从而显着抑制锥虫和肿瘤细胞的生长和活力。此外，5'-（[（（Z）-4-氨基-2-丁烯基]甲基氨基）-5'-脱氧腺苷的乙酰化衍生物确实抑制了HIV-1的生长和感染性，而母体化合物则没有。

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《Journal of Medicinal Chemistry》 |2002年第23期|共11页
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Canio J. Marasco Jr.; Debora L. Kramer; Carl W. Porter; Cyrus J. Bacchi; Donna Rattendi; Louis Kucera; Nathan Iyer; Ralph Bernacki; Paula Pera; Janice R. Sufrin;
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1. Synthesis and Evaluation of Analogues of 5'-([(Z)-4-Amino-2-butenyl]methylamino)-5'-deoxyadenosine as Inhibitors of Tumor Cell Growth, Trypanosomal Growth, and HIV-1 Infectivity [J] . Canio J. Marasco Jr., Debora L. Kramer, Carl W. Porter, Journal of Medicinal Chemistry . 2002,第23期

机译：5'-（[（（Z）-4-氨基-2-丁烯基]甲基氨基）-5'-脱氧腺苷作为肿瘤细胞生长，锥虫生长和HIV-1感染抑制剂的合成和评价
2. Synthesis, molecular modeling and biological evaluation of novel tadalafil analogues as phosphodiesterase 5 and colon tumor cell growth inhibitors, new stereochemical perspective. [J] . Abadi AH, Gary BD, Tinsley HN, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第4期

机译：新型他达拉非类似物作为磷酸二酯酶5和结肠肿瘤细胞生长抑制剂的合成，分子建模和生物学评估，新的立体化学观点。
3. Synthesis and evaluation of 2,7-diamino-thiazolo(4,5-d) pyrimidine analogues as anti-tumor epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. [J] . Lin R, Johnson SG, Connolly PJ, Bioorganic and Medicinal Chemistry Letters . 2009,第8期

机译：2,7-二氨基 - 噻唑（4,5-D）嘧啶类似物作为抗肿瘤表皮生长因子受体（EGFR）酪氨酸激酶抑制剂的合成与评价。
4. Total Paeony Glycoside Inhibits Tumor Growth and Induces Apoptosis in K562 Cells and in S180 Tumor-Bearing Mice [C] . Huiyu Xu, Yanmin Wu, Xiaoqing Luo, Information technology and agricultural engineering . 2011

机译：总Pa药苷抑制K562细胞和S180荷瘤小鼠的肿瘤生长并诱导其凋亡。
5. Design and synthesis of molecular probes to modulate cell membrane permeation: I. Design, synthesis, and biological evaluation of novel chicoric acid analogues as inhibitors of HIV-1 integrase. II. Design, synthesis, and biological evaluation of novel estradiol analogues targeting the membrane estrogen receptor. [D] . Charvat, Trevor Thomas. 2004

机译：设计和合成的分子探针，可调节细胞膜的渗透性：I.设计，合成和生物评价作为抗HIV-1整合酶抑制剂的新型菊苣酸类似物。二。针对膜雌激素受体的新型雌二醇类似物的设计，合成和生物学评估。
6. Synthesis molecular modeling and biological evaluation of novel tadalafil analogues as phosphodiesterase 5 and colon tumor cell growth inhibitors new stereochemical perspective [O] . Ashraf H. Abadi, Bernard D. Gary, Heather N. Tinsley, -1

机译：新型达拉夫尔类似物的合成分子建模与生物学评价为磷酸二酯酶5和结肠肿瘤细胞生长抑制剂新立体化学观点
7. Effects of the S-adenosylmethionine decarboxylase inhibitor, 5'-([(Z)-4-amino-2-butenyl]methylamino)-5'-deoxyadenosine, on cell growth and polyamine metabolism and transport in Chinese hamster ovary cell cultures. [O] . Byers, T L, Wechter, R S, Hu, R H, 1994

机译：S-腺苷甲硫氨酸脱羧酶抑制剂5'-（[[（Z）-4-氨基-2-丁烯基]甲基氨基）-5'-脱氧腺苷对中国仓鼠卵巢细胞培养中细胞生长以及多胺代谢和运输的影响。

Synthesis and Evaluation of Analogues of 5'-([(Z)-4-Amino-2-butenyl]methylamino)-5'-deoxyadenosine as Inhibitors of Tumor Cell Growth, Trypanosomal Growth, and HIV-1 Infectivity

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