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Biochemical pharmacology, metabolism, and mechanism of action of L-alanosine, a novel, natural antitumor agent. 新型天然抗肿瘤药物l -丙氨酸的生化药理学、代谢及作用机制。
Pub Date : 1984-01-01 DOI: 10.1016/s1054-3589(08)60265-3
A K Tyagi, D A Cooney
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引用次数: 19
The pharmacology of prodrugs of 5-fluorouracil and 1-beta-D-arabinofuranosylcytosine. 5-氟尿嘧啶和1- β - d -阿拉伯糖脲基胞嘧啶前药的药理学研究。
Pub Date : 1984-01-01 DOI: 10.1016/s1054-3589(08)60264-1
A F Hadfield, A C Sartorelli
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引用次数: 26
Computer-assisted structure-activity correlations. 计算机辅助构效关系。
Pub Date : 1984-01-01 DOI: 10.1016/s1054-3589(08)60266-5
M Nasr, K D Paull, V L Narayanan

Several types of Michael acceptors, including alpha,beta-unsaturated ketones, lactones, and lactams, have been extensively studied as potential anticancer agents. A concerted effort was made to explore the relationship between the structures of these compounds and their antitumor activity against P388 and L1210 leukemias. This article describes the computer-assisted structure-activity evaluation of more than 14,000 compounds, representing different classes of Michael acceptors, in the NCI file. In this study, advantage has been taken of the computer's ability to search substructures according to precise definitions and to manipulate these substructures utilizing Boolean logic. Olefinic conjugated Michael-type acceptors, e.g., styrenes with different activating groups, cinnamic acid derivatives, and alpha,beta-unsaturated nitro, cyano, sulfone, sulfoxide, and acetylenic compounds, have shown appreciable activity against P388 lymphocytic leukemia. The analysis of lactones and lactams includes substructures representing a wide variety of exocyclic and endocyclic alpha,beta-unsaturated compounds. The analysis describes the effect of certain groups, such as an --OH, --OR, alpha,beta-unsaturated ester, or epoxide, adjacent to the alpha,beta-unsaturated center, on the antitumor activity of these compounds. A combination of one or more of these activating groups with an alpha-methylene-gamma-lactone moiety significantly enhanced the activity against P388. In general, many of the classes of compounds studied have shown poor activity against the more stringent L1210 lymphoid leukemia.

几种类型的迈克尔受体,包括α、β -不饱和酮、内酯和内酰胺,作为潜在的抗癌药物被广泛研究。我们共同努力探索这些化合物的结构与它们对P388和L1210白血病的抗肿瘤活性之间的关系。本文描述了在NCI文件中代表不同类别的Michael受体的14,000多个化合物的计算机辅助结构-活性评估。在这项研究中,利用计算机的优势,根据精确的定义搜索子结构,并利用布尔逻辑操纵这些子结构。烯烃共轭迈克尔型受体,如具有不同活化基团的苯乙烯、肉桂酸衍生物和α、β -不饱和硝基、氰基、砜、亚砜和乙基化合物,对P388淋巴细胞白血病显示出明显的活性。内酯和内酰胺的分析包括代表各种各样的外环和内环α, β不饱和化合物的亚结构。该分析描述了某些基团,如-OH, -OR, α, β -不饱和酯或环氧化物,邻近α, β -不饱和中心,对这些化合物的抗肿瘤活性的影响。一个或多个这些活化基团与α -亚甲基- γ -内酯片段的组合显著增强了对P388的活性。总的来说,许多被研究的化合物对更严重的L1210淋巴细胞白血病的活性都很差。
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引用次数: 13
Current NCI preclinical antitumor screening in vivo: results of tumor panel screening, 1976-1982, and future directions. 当前NCI临床前体内抗肿瘤筛查:1976-1982年肿瘤组筛查结果及未来方向。
Pub Date : 1984-01-01 DOI: 10.1016/s1054-3589(08)60263-x
J M Venditti, R A Wesley, J Plowman
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引用次数: 96
Praziquantel. 吡喹酮。
Pub Date : 1984-01-01 DOI: 10.1016/s1054-3589(08)60268-9
E Groll
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引用次数: 2
The sugar alcohols: a profile. 糖醇:简介。
Pub Date : 1984-01-01 DOI: 10.1016/s1054-3589(08)60267-7
A Jori
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引用次数: 3
The interaction of cancer chemotherapy agents with mononuclear phagocytes. 肿瘤化疗药物与单核吞噬细胞的相互作用。
Pub Date : 1982-01-01 DOI: 10.1016/s1054-3589(08)60020-4
A Mantovani
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引用次数: 23
Development of radiosensitizers: a medicinal chemistry perspective. 放射增敏剂的发展:药物化学的观点。
Pub Date : 1982-01-01 DOI: 10.1016/s1054-3589(08)60023-x
V L Narayanan, W W Lee
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引用次数: 15
The effects of antineoplastic therapy on growth and development in children. 抗肿瘤治疗对儿童生长发育的影响。
Pub Date : 1982-01-01 DOI: 10.1016/s1054-3589(08)60024-1
U Bode, A Oliff
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引用次数: 2
Chloroethylnitrosourea cancer chemotherapeutic agents. 氯乙基亚硝基脲类癌症化疗药物。
Pub Date : 1982-01-01 DOI: 10.1016/s1054-3589(08)60019-8
R J Weinkam, H S Lin
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引用次数: 30
期刊
Advances in pharmacology and chemotherapy
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