Thesis (Ph. D. in Chemistry)--University of California, Berkeley, October 1958. / Part II of the thesis "high intensity light sources" see UCRL-8509. "UCRL-8508" Includes bibliographical references : p. 98-100.

Proefschrift--Groningen. / English summary. "Literatuuroverzicht": p. [3]-10.

No description available.

No description available.

Yes / Aldehyde dehydrogenases (ALDHs) are overexpressed in various tumor types including prostate cancer and considered a potential target for therapeutic intervention. 4-(Diethylamino)benzaldehyde (DEAB) has been extensively reported as a pan-inhibitor of ALDH isoforms, and here, we report on the synthesis, ALDH isoform selectivity, and cellular potencies in prostate cancer cells of 40 DEAB analogues; three analogues (14, 15, and 16) showed potent inhibitory activity against ALDH1A3, and two analogues (18 and 19) showed potent inhibitory activity against ALDH3A1. Significantly, 16 analogues displayed increased cytotoxicity (IC50 = 10-200 μM) compared with DEAB (>200 μM) against three different prostate cancer cell lines. Analogues 14 and 18 were more potent than DEAB against patient-derived primary prostate tumor epithelial cells, as single agents or in combination treatment with docetaxel. In conclusion, our study supports the use of DEAB as an ALDH inhibitor but also reveals closely related analogues with increased selectivity and potency. / S12-027/PCUK_/Prostate Cancer UK/United Kingdom

Call number: LD2668 .T4 1978 C52 / Master of Science

published_or_final_version / Chemistry / Doctoral / Doctor of Philosophy

published_or_final_version / abstract / Chemistry / Doctoral / Doctor of Philosophy

The initial aim of this research project was to oxidise Cr C4 alcohols to their respective aldehydes. However, isolation of these aldehydes was impossible due to their low boiling points. Another problem was the proximity of the boiling points of these aldehydes with the boiling points of solvents used in reactions. As a result, the alcohols investigated in this project were changed to C4-C6 alcohols. Different oxidising reagents are known that oxidise oxidise primary alcohols to aldehydes. Of these, chromium (VI) has been used the most. In this project, Chromium (VI) supported on different inert: inorganic supports was chosen as the oxidising reagent. The first task was therefore to synthesise these supported oxidants. The synthesis of some of these oxidants was lengthy. This is advantage the preparation of supported oxidants. Unsupported oxidants like PCC and chromium trioxide were only used as a basis of comparison to emphasise the usefulness of supported oxidants. Pyridinium chlorochromate was used to oxidise primary alcohols to aldehydes in moderate yields. The reaction was found to be moisture sensitive. The yield and the duration of the reaction was found to be better with the use of molecular sieves. Silica gel-supported pyridinium chromate was also used to oxidise alcohols to aldehydes in good yields. Poly[vinyl(pyridinium chlorochromate)] was used to oxidise I-hexanol and I-pentanol to their respective aldehydes also in good yields. The duration of these reactions ranged from 30 min. to 3 days. During the oxidation of alcohols using silica gel-supported chromium trioxide and diethyI ether/chromium trioxide it was found that the reaction conditions can be changed so that either aldehydes or symmetrical esters were the products. This was achieved by varying the duration of the reaction. Silica gel-supported chromium trioxide resulted in both the aldehydes and esters in good yields while the diethyl iii Aluminium-supported chromium trioxide, kieselguhr-supported chromic acid, alumium silicate-supported chromic acid and alumina-supported pyridinium chlorochromate were used to oxidise primary alcohols to symmetrical and unsymmetrical esters in good to excellent yields. The duration of these reactions varied from 1 hour to 48 hours depending on the conditions employed and the chain length of the reagents. / Thesis (M.Sc.)-University of Natal, Pietermaritzburg, 1998.

The research presented herein is concerned with the exploration of tandem processes initiated by the conjugate reduction of Michael acceptors, encompassing the asymmetric reductive Dieckmann reaction and the two-carbon homologation of aldehydes by two complementary methodologies. Chapter 1 introduces the area of transition metal catalysed tandem reductive processes as a tool for carbon-carbon bond formation. An extensive discussion of this methodology is included and recent advances in the area are highlighted. Chapter 2 discusses the initial study into the asymmetric reductive Dieckmann condensation. 3,3’-Disubstituted 4-oxopyrrolidines were synthesised in up to 93% ee using both molybdenum and copper catalysis. Chapter 3 describes the novel molybdenum-catalysed two-carbon homologation of aldehydes by the reduction of alkylidene Meldrum’s acid derivatives. No over reduction to the corresponding alcohol is observed, as the aldehyde functionality remains protected until hydrolysis. Chapter 4 discusses the mild, expeditious amine promoted reduction of cyclic malonates to β-substituted propionaldehydes. The synthetic utility of the methodology is demonstrated by the synthesis of γ-substituted propylamines in a one-pot hydrosilylation/reductive amination process. Chapter 5 describes the synthesis and characterisation for the compounds discussed in chapters 2, 3 and 4.