Prof. Dr. Adam Daïch

University: Le Havre University
Department: Department of Organic Chemistry
Research Fields: * Chemistry of iminium, acylium and N-acyliminium ions alone or in tandem with known reactions. Particular attention is paid on heterocyclization process using N, O, S and Se heteroatoms as internal nucleophiles. * Synthesis of fused pyrrolidone and isoindolone heterocyclic systems including alkaloid derivatives, peptidomimetics and products with NCS activity. * Synthesis of cytotoxic and anti-cancer analogues of the topoisomerase-I poisons Camptothecin, Aromathecin and Luotonine-A. Use of N-acyliminium chemistry in tandem with Friedel-Crafts reaction. * Elaboration of new tandem and cascade synthetic methodology to accede natural and unnatural spiroindole-heterocycles. Synthesis and evaluation of their Biological properties. * Asymmetric synthesis of polyhydroxylated alkylindolizidines as new potentially inhibitors of glycosidases using furan, thiophene and benzo[b]thiophene rings as alkyl and/or arylalkyl source.

Publications

1 Synthesis of Analogue to Camptothecine

Authors: Abdulkareem Hamid, Adam Daïch

Abstract:

Camptothecin (CPT) is a cytotoxic quinoline alkaloid, which inhibits the DNA enzyme topoisomerase I (topo I). It was discovered in 1966 by M. E. Wall and M. C. Wani in systematic screening of natural products for anticancer drugs. It was isolated from the bark and stem of Camptotheca acuminata (Camptotheca, Happy tree), a tree native in China. CPT showed remarkable anticancer activity in preliminary clinical trials but also low solubility and (high) adverse drug reaction. Because of these disadvantages synthetic and medicinal chemists have developed numerous syntheses of Camptothecine [1][2][3] and various derivatives to increase the benefits of the chemical, with good results. In our method CPT analogues has be six steps starting from available material DL Malic acid.

Keywords: Synthesis, analogue, Camptothecine

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Abstracts

1 New Method for the Synthesis of Different Pyrroloquinazolinoquinolin Alkaloids

Authors: Abdulkareem M. Hamid, Yaseen Elhebshi, Adam Daïch

Abstract:

Luotonins and its derivatives (Isoluotonins) are alkaloids from the aerial parts of Peganum nigellastrum Bunge that display three major skeleton types. Luotonins A, B, and E are pyrroloquinazolinoquinoline alkaloids. A few methods were known for the sysnthesis of Isoluotonin. All luotonins have shown promising cytotoxicities towards selected human cancer cell lines, especially against leukemia P-388 cells. Luotonin A is the most active one, with its activity stemming from topoisomerase I-dependent DNA-cleavage. Such intriguing biological activities and unique structures have led not only to the development of synthetic methods for the efficient synthesis of these compounds, but also to interest in structural modifications for improving the biological properties. Recent progress in the study of luotonins is covered.

Keywords: Alkaloids, luotonin A, isoluotonin, pyrroloquiolines

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