Kryshchyshyn A. Synthesis and biological activity of chromeno[4',3':4,5]thiopyrano[2,3-d]thiazole and isothiochromeno[4a,4-d]thiazole derivatives

Українська версія

Thesis for the degree of Candidate of Sciences (CSc)

State registration number

0411U003758

Thesis Registration Form

0411U003758.pdf

Applicant for

Specialization

  • 15.00.02 - Фармацевтична хімія та фармакогнозія

13-05-2011

Specialized Academic Board

Д 35.600.02

Danylo Halytsky Lviv National Medical University

Essay

Object - [2+3]-cyclocondansation processes in the synthesis of 4-thiazolidones, thiazolidone derivatives condensation by methylen-active group in the position 5, thionation reactions, heterodiene synthesis, alkylation, cyanoetylation, acylation reactions, tandem "domino" porcesses; aim - synthesis of new chromeno[4',3':4,5]thiopyrano[2,3-d]thiazoles and isothiochromeno[4a,4-d]thiazoles, searching of effective and nontoxic substances with anticancer, antimicobacterial and antiparasitic activities among them; methods - organic synthesis, mass-spectrometry, NMR-spectroscopies, X-ray analysis, elemental analysis, pharmacological screening, QSAR-analysis, docking, molecular biological research; novelty - methods of synthesis and transformations of new chromeno[4',3':4,5]thiopyrano[2,3-d]thiazoles and isothiochromeno[4a,4-d]thiazoles are carried out, biological activity of synthesized compounds is investigated, for the first time experimental confirmation of anticancer activity realization through receptor-mediated apoptosis induction is obtained; the outcomes - "domino" Knoevenagel- and thionation-hetero-Diels-Alder reactions are investigated, highly active substances with anticancer, antimicobacterial and antiparasitic activities are identified.Bbased on experimental and in silico data the recommendations for design of thiopyrano[2,3-d]thiazole derivatives as anticancer agents are proposed; these were introduced into scientific and educational processes of Zaporizzhia State Medical University, National Pharmaceutical University, National University "Lviv Politechnic"; area - pharmacy.

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Dysertacija_Kryshchyshyn--Dodatky--Dodatok1.doc

Dysertacija_Kryshchyshyn--Dodatky--Додаток 2.doc

Dysertacija_Kryshchyshyn--References.doc

Dysertacija_Kryshchyshyn--Rozdil-1--Rozdil-1.doc

Dysertacija_Kryshchyshyn--Rozdil-2--2-text.doc

Dysertacija_Kryshchyshyn--Rozdil-2--Table 2.5.doc

Dysertacija_Kryshchyshyn--Rozdil-2--Table2.1.doc

Dysertacija_Kryshchyshyn--Rozdil-2--table2.2.doc

Dysertacija_Kryshchyshyn--Rozdil-2--table2.6.doc

Dysertacija_Kryshchyshyn--Rozdil-3--3-text.doc

Dysertacija_Kryshchyshyn--Rozdil-3--table3.1.doc

Dysertacija_Kryshchyshyn--Rozdil-3--table3.2.doc

Dysertacija_Kryshchyshyn--Rozdil-3--table3.3.doc

Dysertacija_Kryshchyshyn--Rozdil-3--table3.4.doc

Dysertacija_Kryshchyshyn--Rozdil-3--table3.5.doc

Dysertacija_Kryshchyshyn--Rozdil-3--table3.6.doc

Dysertacija_Kryshchyshyn--Rozdil-3--table3.7.doc

Dysertacija_Kryshchyshyn--Rozdil-4--table 4.7-4.9.doc

Dysertacija_Kryshchyshyn--Rozdil-4--table_4.10.doc

Dysertacija_Kryshchyshyn--Rozdil-4--table_4.12.doc

Dysertacija_Kryshchyshyn--Rozdil-4--table_4.2.doc

Dysertacija_Kryshchyshyn--Rozdil-4--table_4.3.doc

Dysertacija_Kryshchyshyn--Rozdil-4--text_4.doc

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