• Title/Summary/Keyword: Unreported

Search Result 224, Processing Time 0.022 seconds

Potential Antitumor $\alpha$-Methylene-$\gamma$-butyrolactone-Bearing Nucleic Acid Base. 3. Synthesis of $5^1$-Methyl-$5^1$-[(6-substituted-9H-purin-9-yl)methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofurans

  • Kim, Jack-C.;Kim, Si-Hwan;Kim, Ji-A;Choi, Soon-Kyu;Park, Won-Woo
    • Archives of Pharmacal Research
    • /
    • v.21 no.4
    • /
    • pp.458-464
    • /
    • 1998
  • Search for a new $\alpha$-methylene-$\gamma$-butyrolactone-bearing 6-substituted purine as a potental antitumor agent has led to synthesize seven, hitherto unreported, $5^1$-Methyl-$5^1$-[(6-substituted-9H-purin-9-yl)methyl]-$2^1$-oxo-$3^1$- methylenetetrahydrofurans (H, Cl, l, $CH_3$, $NH_2$, SH, >C=O) (6a-g). These include $5^1$-Methyl-$5^1$-[(9H-purin-9-yl)methyll-$2^1$-oxo-$3^1$ -methylenetetrahydrofurans (6a), $5^1$-Methyl-$5^1$-[(6-chloro-9H-purin-9-yl)methyl]-$2^1$-oxo-$3^1$-methylenetetrahydr ofurans (6b), $5^1$-Methyl-$5^1$-[(6-chloro-9H-purin-9-yl) methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6c), $5^1$-Methyl-$5^1$-[(6-methyl-9H-purin-9-yl) methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6d), $5^1$-Methyl-$5^1$-[(9H-adenin-9-yl)methyll-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6e), $5^1$-Methyl-$5^1$-[(6-mercapto-9H-purin-9-yl) methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6f) and $5^1$-Methyl-$5^1$-[(9H-hypoxanthin-9-yl)methyll-$2^1$-oxo-$3^1$-methylenetetrahydrof urans (6g) which were made by the Reformatsky-type reaction of ethyl $\alpha$-(bromomethyl) acrylate with the corresponding (6-substituted-9H-purin-9-yl)-2-propanone intermediates (5a-g). These ketone intermediates 5a-g, 1-(9H-purin-9-yl)-2-propanone (5a), 1-(6-chloro-9H-purin-9-yl)-2-propanone (5b), 1-(6-iodo-9H-purin-9-yi)-2-propanone (5c), 1-(6-methyl-9H-purin-9-yl)-2-propanone (5d), 1-(9H-adenin-9-yl)-2-propanone (Se), 1-(6-mercapto-9H-purin-9-yl)-2-propanone (5f), and 1-(9H-hypoxanthin-9-yl)-2-propanone (5g) were directly obtained by the alkylation of the 6-substituted purine bases with the chloroacetone in the presence of $K_2$$CO_3$ (or NaH) under DMF (or DMSO). The preliminary in vitro cytotoxcity assay for the synthetic .alpha.-methylene-y-butyro-lactone compounds (6a-g) were determined against three cell lines (PM-3A, P-388, and K-562) and showed the moderate antitumor activity ($IC_50$ ranged from 1.4 to 4.3 $\mu\textrm{g}$/ml) with the compound $5^1$-methyl-$5^1$ -[(9H-hypoxanthin-9-yl)methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofuran (6g) showing the least antitumor activity.

  • PDF

Compensation Criteria for Investigation Services and Strengthening Normative Force Plans for Detailed Qualification Criteria for Examination of Archaeological Heritage (매장문화재 조사용역 대가기준과 적격심사 세부기준 제도의 규범력 강화 방안)

  • Choi, Min-jeong
    • Korean Journal of Heritage: History & Science
    • /
    • v.52 no.2
    • /
    • pp.240-253
    • /
    • 2019
  • Archaeological heritages are precious cultural relics and public assets that must be preserved, conserved, and shared with people all over the world. Investigating archaeological heritage is valuable and plays an important role for the public good; our ancestors' cultures can be restored, and it helps with developing a clear understanding of the cultural and social aspects of a historical period as well as teaches about historical factors unreported in the literature. One of the most basic and important conditions necessary for recognizing the value and importance of archaeological heritage investigation, expertise, and quality improvement is to establish detailed criteria for investigation services and the qualification examination of archaeological heritage. Observation of detailed criteria and the qualification examination of archaeological heritage can partially demonstrate society's recognition of strengthening transparency, public property, and the objectivity of the investigation of archaeological heritage. However, the detailed criteria for investigation services and the qualification examination of archaeological heritage currently implemented as administrative rules are neither followed by all institutes in the public and private sectors nor the government. Thus, there are serious problems in terms of the effectiveness and stability of institutions. The detailed criteria for the qualification examination breach the principle of statutory reservation, the principle of statutory regulation, and regulations on the announcement and management of orders and rules. Non-compliance with compensation criteria for investigation services or with detailed criteria for the qualification examination of archaeological heritage will be one of the reasons for the failure of the investigation foundation for archaeological heritage in the future. That is, it will result in the expansion, reproduction, and repetition of a vicious cycle of conflict between developers, who are the decision-makers responsible for selecting an investigating organization for archaeological heritage and determining the cost, and investigating organizations. This includes the impractical shortening of investigation periods and reducing costs by developers, distrust of the values and the importance of investigations of archaeological heritage, a decrease in quality, accidents caused by a lack of safety, a lack of occupational ethics, and non-recruitment of new experts, etc. Therefore, it is necessary to change the structure from a vicious cycle to a virtuous cycle, and promote the enactment of regulations that will ensure effectiveness and stability in the process of attaining the goals of the institution and application of the institution, as well as the continuous advancement of work to fill the gaps with reality.

Cellulose degrading basidiomycetes yeast isolated from the gut of grasshopper in Korea (한국의 메뚜기의 장에서 분리된 Cellulose를 분해하는 담자균 효모)

  • Kim, Ju-Young;Jang, Jun Hwee;Park, Ji-Hyun;Jung, Hee-Young;Park, Jong-Seok;Cho, Sung-Jin;Lee, Hoon Bok;Limtong, Savitree;Subramani, Gayathri;Sung, Gi-Ho;Kim, Myung Kyum
    • Korean Journal of Microbiology
    • /
    • v.54 no.4
    • /
    • pp.362-368
    • /
    • 2018
  • Grasshoppers play vital role in the digestion of photosynthetically fixed carbons. With the aid of intestinal microflora, the grasshopper can degrade leaves constituents such as cellulose and hemicellulose. The purpose of this study was to examine cellulolytic yeast isolates from the gut of grasshoppers collected in Gyeonggi Province, South Korea. Among the yeast isolates, ON2, ON17 (two strains), and ON6 (one strain) showed positive cellulolytic activity in the CMC-plate assay. The sequence analyses of D1/D2 domains of the large subunit rDNA gene and the internal transcribed spacer (ITS) regions revealed that the strains ON2 and ON17 were most closely related to Papiliotrema aspenensis CBS $13867^T$ (100%, sequence similarity in D1/D2 domains; 99.4% sequence similarity in ITS) and strain ON6 related to Saitozyma flava (100% in D1/D2 domains; 99.0% in ITS). All these three yeast strains are capable of degrading cellulose; therefore, the members of endosymbiotic yeasts may produce their own enzymes for carbohydrate degradation and convert mobilized sugar monomers to volatile fatty acids. Thus, the endosymbiotic yeast strains ON2, ON17 (represents the genus Papilioterma) and ON6 (Saitozyma) belonging to the family Tremellomycetes, are unreported strains in Korea.

A Study on the Present Condition and Improvement of Cultural Heritage Management in Seoul - Based on the Results of Regular Surveys (2016~2018) - (서울특별시 지정문화재 관리 현황 진단 및 개선방안 연구 - 정기조사(2016~2018) 결과를 중심으로 -)

  • Cho, Hong-seok;Suh, Hyun-jung;Kim, Ye-rin;Kim, Dong-cheon
    • Korean Journal of Heritage: History & Science
    • /
    • v.52 no.2
    • /
    • pp.80-105
    • /
    • 2019
  • With the increasing complexity and irregularity of disaster types, the need for cultural asset preservation and management from a proactive perspective has increased as a number of cultural properties have been destroyed and damaged by various natural and humanistic factors. In consideration of these circumstances, the Cultural Heritage Administration enacted an Act in December 2005 to enforce the regular commission of surveys for the systematic preservation and management of cultural assets, and through a recent revision of this Act, the investigation cycle has been reduced from five to three years, and the object of regular inspections has been expanded to cover registered cultural properties. According to the ordinance, a periodic survey of city- or province-designated heritage is to be carried out mainly by metropolitan and provincial governments. The Seoul Metropolitan Government prepared a legal basis for commissioning regular surveys under the Seoul Special City Cultural Properties Protection Ordinance 2008 and, in recognition of the importance of preventive management due to the large number of cultural assets located in the city center and the high demand for visits, conducted regular surveys of the entire city-designated cultural assets from 2016 to 2018. Upon the first survey being completed, it was considered necessary to review the policy effectiveness of the system and to conduct a comprehensive review of the results of the regular surveys that had been carried out to enhance the management of cultural assets. Therefore, the present study examined the comprehensive management status of the cultural assets designated by the Seoul Metropolitan Government for three years (2016-2018), assessing the performance and identifying limitations. Additionally, ways to improve it were sought, and a DB establishment plan for the establishment of an integrated management system under the auspices of the Seoul Metropolitan Government was proposed. Specifically, survey forms were administered under the Guidelines for the Operation of Periodic Surveys of National Designated Cultural Assets; however, the types of survey forms were reclassified and further subdivided in consideration of the characteristics of the designated cultural assets, and manuals were developed for consistent and specific information technologies in respect of the scope and manner of the survey. Based on this analysis, it was confirmed that 401 cases (77.0%) out of 521 cases were generally well preserved; however, 102 cases (19.6%) were found to require special measures such as attention, precision diagnosis, and repair. Meanwhile, there were 18 cases (3.4%) of unsurveyed cultural assets. These were inaccessible to the investigation at this time due to reasons such as unknown location or closure to the public. Regarding the specific types of cultural assets, among a total of 171 cultural real estate properties, 63 cases (36.8%) of structural damage were caused by the failure and elimination of members, and 73 cases (42.7%) of surface area damage were the result of biological damage. Almost all plants and geological earth and scenic spots were well preserved. In the case of movable cultural assets, 25 cases (7.1%) among 350 cases were found to have changed location, and structural damage and surface area damage was found according to specific material properties, excluding ceramics. In particular, papers, textiles, and leather goods, with material properties that are vulnerable to damage, were found to have greater damage than those of other materials because they were owned and managed by individuals and temples. Thus, it has been confirmed that more proactive management is needed. Accordingly, an action plan for the comprehensive preservation and management status check shall be developed according to management status and urgency, and the project promotion plan and the focus management target should be selected and managed first. In particular, concerning movable cultural assets, there have been some cases in which new locations have gone unreported after changes in ownership (management); therefore, a new system is required to strengthen the obligation to report changes in ownership (management) or location. Based on the current status diagnosis and improvement measures, it is expected that the foundation of a proactive and efficient cultural asset management system can be realized through the establishment of an effective mid- to long-term database of the integrated management system pursued by the Seoul Metropolitan Government.