2-(4-Chlorobenzyl)-6-arylimidazo2,1-b]1,3,4]thiadiazoles: Synthesis, cytotoxic activity and mechanism of action

The cytotoxic activity of a new series of 2-(4'-chlorobenzyl)-5,6-disubstituted imidazo2,1-b]1,3,4]wthiadiazoles against different human and murine cancer cell lines is reported. Among the tested compounds, two derivatives namely 2-(4-chlorobenzyl)-6-(2-oxo-2H-chromen-3-yl)imidazo2,1-1)]1,3,4]th iadiazole-5-carbaldehyde 4i and 2-(4-chlorobenzyl)-6-(2-oxo-2H-chromen-3-ypimidazo2,1-1)]1,3,4]thi adiazol-5-yl thiocyanate 5i emerged as the most potent against all the cell lines. To investigate the mechanism of action, we selected compounds 4i for cell cycle study, analysis of mitochondrial membrane potential and Annexin V-FITC flow cytometric analysis and DNA fragmentation assay. Results showed that 4i induced cytotoxicity by inducing apoptosis without arresting the cell cycle. (C) 2014 Elsevier Masson SAS. All rights reserved.

Synthesis and antiproliferative activity of imidazo2,1-b]1,3,4]thiadiazole derivatives

A series of 2,5,6-substituted imidazo2,1-b]1,3,4]thiadiazole derivatives have been prepared and were tested for antiproliferative activity on cancer cells at the National Cancer Institute. Results showed that molecules with a benzyl group at position 2, exhibited an increase in activity for the introduction of a formyl group at the 5 position. The compound 2-benzyl-5-formyl-6-(4-bromophenyl)imidazo 2,1-b]1,3,4]thiadiazole 22 has been chosen for understanding the mechanism of action by various molecular and cellular biology studies. Results obtained from cell cycle evaluation analysis, analysis of mitochondrial membrane potential and Annexin V-FITC by flow cytometric analysis, ROS production and expression of apoptotic and DNA-repair proteins suggested that compound 22 induced cytotoxicity by activating extrinsic pathway of apoptosis, however, without affecting cell cycle progression. (C) 2014 Elsevier Ltd. All rights reserved.

One-step synthesis of a cyclic 2,17-dioxo3,3](4,4 `)biphenylophane and first preparation of a microporous polymer network from a macrocyclic precursor by cyclotrimerization

One-step synthesis of a cyclic 2,17-dioxo3,3](4,4') biphenylophane (MC) was achieved in high yield; its structure was verified by single crystal X-ray analysis. As a first example, a microporous polymer network was formed from macrocycle MC via acid-catalysed cyclotrimerization yielding a BET surface area of ca. 570 m(2) g(-1).

Synthesis and evaluation of 2,5-di(4-aryloylaryloxymethyl)-1,3,4-oxadiazoles as anti-cancer agents

A series of 2,5-di(4-aryloylaryloxymethyl)-1,3,4-oxadiazoles 9a-j were obtained via multistep synthesis from hydroxybenzophenones 4a-e. The cytotoxicity of compounds 9a-j was evaluated against human leukemia cell lilies (K562 and CEM). The compounds exhibited moderate to good anti-cancer activity with compounds 9b and 9i having a chloro group exhibiting the best activity (IC50 = 10 mu M). Compound 9i exhibited activity against both the cell lines and 9b only exhibited activity against CEM. Further, a lactate dehydrogenase (LDH) assay and DNA fragmentation studies of the compounds 9a-j were also performed. (C) 2013 Elsevier Masson SAS. All rights reserved.

Synthesis of Optically Active 2-Amino-1,3,4-oxadiazoles and their Hybrid Peptides

Synthesis of 2-amino-1,3,4-oxadiazole derivatives of N-Cbz(benzyloxycarbonyl)/Boc-protected amino/peptide acids under sonication is described. The conditions involved in the present protocol are simple, mild, and racemization free. The utility of 2-amino group in the substituted oxadiazoles for the incorporation of peptide and ureido bonds to obtain hybrid peptidomimetics is also delineated. The 2-amino-1,3,4-oxadiazole 3b was obtained as a single crystal, and its molecular structure has been confirmed through X-ray crystallographic study.

Crystal chemistry and photomechanical behavior of 3,4-dimethoxycinnamic acid: correlation between maximum yield in the solid-state topochemical reaction and cooperative molecular motion

A new monoclinic polymorph, form II (P2(1)/c, Z = 4), has been isolated for 3,4-dimethoxycinnamic acid (DMCA). Its solid-state 2 + 2 photoreaction to the corresponding alpha-truxillic acid is different from that of the first polymorph, the triclinic form I (P (1) over bar, Z = 4) that was reported in 1984. The crystal structures of the two forms are rather different. The two polymorphs also exhibit different photomechanical properties. Form I exhibits photosalient behavior but this effect is absent in form II. These properties can be explained on the basis of the crystal packing in the two forms. The nanoindentation technique is used to shed further insights into these structure-property relationships. A faster photoreaction in form I and a higher yield in form II are rationalized on the basis of the mechanical properties of the individual crystal forms. It is suggested that both Schmidt-type and Kaupp-type topochemistry are applicable for the solid-state trans-cinnamic acid photodimerization reaction. Form I of DMCA is more plastic and seems to react under Kaupp-type conditions with maximum molecular movements. Form II is more brittle, and its interlocked structure seems to favor Schmidt-type topochemistry with minimum molecular movement.

以1-苯基-3-甲基-4-苯甲酰基代吡唑酮[5]萃取稀土和钍铀钛锆及其在分析化学中的某些应用

本文研究了以PMBP-苯萃取稀土和钍、铀、钛、锆的萃取行为。测定了La、Ce、Pr、Nd、Sm、Gd、Dy、Yb、Y、U(Ⅵ)、Ti、Th和Zr的pH_(1/2)值,计算了它们的萃取平衡常数。并介绍了近十年来作者将此萃取剂应用于铀、钍、稀土、鋰、钢铁合金及岩石中痕量稀土、钍和钙的分离和测定方面的工作。实践证明,PMOP合成简便、价格低廉、萃取能力较强,是比TTA更为优越的萃取剂。

Financing And Cooperation For Sustainable Development In The Mediterranean, Sophia Antipolis, France, 3-4 June 2004: Volume II: Technical Report of the Workshop

(263 page document)

Proceedings of the Seventh U.S.-Japan Meeting on Aquaculture, Marine Finfish Culture, Tokyo, Japan, October 3-4, 1978

The United States and Japanese counterpart panels on aquaculture were formed in 1969 under the United States-Japan Cooperative Program in Natural Resources (UJNR). The panels currently include specialists drawn from the federal departments most concerned with aquaculture. Charged with exploring and developing bilateral cooperation, the panels have focused their efforts on exchanging information related to aquaculture which could be of benefit to both countries. The UJNR was started by a proposal made during the Third Cabinet-Level Meeting of the Joint United States-Japan Committee on Trade and Economic Affairs in January 1964. In addition to aquaculture, current subjects in the program are desalination of seawater, toxic microorganisms, air pollution, energy, forage crops, national park management, mycoplasmosis, wind and seismic effects, protein resources, forestry, and several joint panels and committees in marine resources research, development, and utilization. Accomplishments include: Increased communications and cooperation among technical specialists; exchanges of information, data, and research findings; annual meetings of the panels, a policy coordinative body;' administration staff meetings; exchanges of equipment, materials, and samples; several major technical conferences; and beneficial effects on international relations.(PDF file contains 37 pages.)

II Materialen Zientzia eta Teknologia Kongresua. Donostian, 2014 uztailak 3, 4

Egurra, sua; zura, mahaia; larrua, abarka; artila, galtzerdia; burnia, ardatza; altzairua, iltzea; buztina, teila; porlana, pareta; galipota, kaminoa… Materialak, tresnak. Zenbat aldiz aipatuak Euskal Herriko eguneroko berbeta, hizketa eta solasaldi arruntetan! Harria, herria, zioen Aresti poetak ere. Teknologiaren alorrari dagokionean, materialen gaia gehienbat metalurgiarekin lotu izan zen mundu osoan eta batik bat gure herrian. XX. mendearen hasieran garapen industrialak egundoko bultzada izan zuen, bereziki automobilgintzaren eta hegazkingintzaren hedapenarekin. Halaber, elektrizitatea arras zabaldu zelarik, etxetresnen kontzeptua bera ere aldatu egin zen. Horrela, tresna eta baliabide berriek gizartearen ohituren eta izaera beraren aldaketa sakonak erakarri zituzten. Baina, hori guztia material berriak sortu eta garatzeari zor zitzaion: polimeroak, metal eta zeramika berriak, estaldura sintetikoak, etab. ezinbestekoak bilakatu ziren. Orduan ikusi zen materialek arlo berezi bat merezi zutela zientziaren eremuan. Eta horrela, premiak eraginda, Fisika eta Kimika oinarrizko zientzietatik abiatua eta ingeniaritzaren gorpuzkera sendoaz hornituta, Materialen Zientzia sortu zen. Materialen Zientzia eta Teknologia euskaraz, beranduago etorriko zen. Askoz lehenagokoak dira “Pisia” eta “Kimia”, 1935 inguran Jauregi apaiz karmeldar aitzindariak idatzitako liburuak. Eta gero, iluntasunean bidexka ia ezinezkoak jorratuz, Elhuyar Taldea 1972an, Udako Euskal Unibertsitatea 1973an eta UZEI 1977an sortu ziren; euskara irakaskuntzara, unibertsitatera eta zientziara jalgi zedin. Hurrengo urtetan emaitzak gauzatzen hasiak ziren, bai eta Materialen Zientzia eta Teknologiaren arlo berrian ere. Izan ere, mugarria da, besteen artean, Nafarroako Unibertsitateko Donostiako Goi Mailako Injineru Eskolan 1979an Jon Nazabalek aurkeztu zuen “Zenbait mekanizapen errazeko altzairuren berotako erresistentzia mekanikoa eta duktibilitatea” doktoretzatesia. 1991ko uztailean, Udako Euskal Unibertsitateak “Materialen ezagutza teknika ezberdinen bitartez” topaketa antolatu zuen Iruñean, bertan 30en bat zientzialari euskaldun bildu ginelarik. Gaur egun, Euskal Herrian baditugu hainbat ingeniari, fisikari, kimikari eta biologo euskaldun, Materialen Zientzia eta Teknologia garatzen ari direnak, bai unibertsitate, bai zentro teknologiko eta enpresetan. Pertsona horien interesak, ikuspegiak eta lorpenak euskaraz azaltzeko antolatu zen 2012an Arrasaten Materialen Zientzia eta Teknologia I kongresua, ehunen bat pertsona bilduz. Orain dela bi urte hartutako konpromisoari helduz, eta harian haritik jarraituz, aurten Materialen Zientzia eta Teknologia II kongresua UPV/EHUko Polymat institutuak antolatu du. Aldez aurretik, mila esker dagoeneko parte hartzeko izena eman duten guztiei eta gure esker onenak erakunde laguntzaileei: Euskal Herriko Unibertsitatea, Kutxa, CicNanogune eta Elhuyar. Zientziak eta euskarak elkartzen gaituzte. Eta bietan badago elkartze gune bat: kinka larrian daudela beti. Ez baitago zientziarik zientzialariaren zalantzarik gabe, ez eta euskara euskaldun bakoitzaren nahi pertsonalik barik. Antxon Santamaria, Batzorde Antolatzailearen izenean